General Information of Drug (ID: DMM9X0G)

Drug Name
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info
Synonyms
4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-one; AC-42; CHEMBL1242950; AC42; GTPL289; SCHEMBL4504348; ANTKBACNWQHQJE-UHFFFAOYSA-N; ZINC2022527; BDBM50326219; AKOS030284249; NCGC00485453-01; gamma-(4-Butylpiperidino)-2'-methylbutyrophenone; L019209; 4-(4-butylpiperdin-1-yl)-1-(2-methylphenyl)butan-1-one; 4-(4-butylpiperidin-1-yl)-1-(2-methylphenyl)butan-1-one
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9948320
TTD Drug ID
DMM9X0G

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Patented Agent(s)
Preclinical Drug(s)
Drug(s) Targeting Dopamine D3 receptor (D3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cariprazine DMJYDVK Bipolar disorder 6A60 Approved [4]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [5]
Ropinirole DMA6S1D Parkinson disease 8A00.0 Approved [5]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [6]
P2B-001 DM9PVHX Parkinson disease 8A00.0 Phase 3 [7]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [8]
ONC201 DMM5SCF Endometrial cancer 2C76 Phase 2 [9]
TAK-906 DMBQD9H Diabetic gastroparesis DA41.00 Phase 2 [10]
GSK598809 DMGU05N Drug abuse 6C4G.1Z Phase 2 [11]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Meclinertant DMBIO6E Inflammatory bowel disease DD72 Phase 2/3 [12]
ABS-212 DMZ52P6 Pain MG30-MG3Z Terminated [13]
CGX-1160 DMADYF7 Acute or chronic pain MG30-MG31 Terminated [14]
JMV458 DMC1ARG Discovery agent N.A. Investigative [15]
Neurotensin(8-13) DMOBU62 N. A. N. A. Investigative [16]
JMV449 DME9GF8 Discovery agent N.A. Investigative [17]
SR48527 DMUHQS9 Discovery agent N.A. Investigative [18]
HBN-2 DM5VDU2 Neurological disorder 6B60 Investigative [19]
[3H]meclinertant DMEX6GT Discovery agent N.A. Investigative [18]
H-Arg-Arg-Pro-Tyr-Ile-Aac-OH DMENVKA Discovery agent N.A. Investigative [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pentagastrin DMRCLZB Diagnostic imaging N.A. Approved [21]
Ceruletide DM2WE5K Caerulein stimulated gastric and pancreatic secretion 5A4Y Approved [22]
GASTRAZOLE DMO3ITF Duodenal ulcer DA63 Phase 3 [23]
Dexloxiglumide DM52HUD Pancreatic malfunction DC30-DC3Z Phase 2 [24]
Spiroglumide DM7NJWY Stomach disease DA43-DA4Y Phase 2 [25]
TT-223 DMCDMFP Type-1 diabetes 5A10 Phase 2 [26]
Z 360 DM2M80G Discovery agent N.A. Phase 2 [27]
S-0509 DM4KWEF Ulcerative colitis DD71 Phase 2 [28]
YF-476 DM54MAJ Stomach ulcer DA60.Z Phase 2 [29]
Itriglumide DM5UFRO Anxiety disorder 6B00-6B0Z Phase 2 [30]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lofexidine DM1WXA6 Heroin and opiate withdrawal 6C43 Approved [31]
MOXONIDINE DMGFB0E Alcohol dependence 6C40.2 Approved [32]
Connexyn DMF29Q5 Attention deficit hyperactivity disorder 6A05.Z Approved [33]
Guanfacine DMPN5IH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [34]
A295 DM55GO2 Aggressive cancer 2A00-2F9Z IND submitted [35]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [36]
DSP-1200 DM4WSHG Depression 6A70-6A7Z Phase 1 [8]
MAZAPERTINE DMRHYAU N. A. N. A. Discontinued in Phase 2 [37]
NMI-870 DMU596F Sexual dysfunction HA00-HA01 Discontinued in Phase 2 [38]
SNAP-5089 DMROJEN Heart arrhythmia BC65 Terminated [39]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [40]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [41]
Tropicamide DM1D90W Mydriasis LA11.62 Approved [42]
Diphenidol DMHPWOM Nausea MD90 Approved [43]
A-987306 DMU34BK Discovery agent N.A. Investigative [44]
ISOCLOZAPINE DM52CPU Discovery agent N.A. Investigative [45]
FLUMEZAPINE DMW0HOG Discovery agent N.A. Investigative [46]
ISOLOXAPINE DMH1BN4 Discovery agent N.A. Investigative [47]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester DMVEH40 Discovery agent N.A. Investigative [41]
GNF-PF-5618 DMT8VUS Discovery agent N.A. Investigative [48]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [49]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [50]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [51]
Desipramine DMT2FDC Attention deficit hyperactivity disorder 6A05.Z Approved [49]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [52]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [53]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [54]
Venlafaxine DMR6QH0 Anxiety disorder 6B00-6B0Z Approved [53]
Trimipramine DM1SC8M Major depressive disorder 6A70.3 Approved [55]
Duloxetine DM9BI7M Depression 6A70-6A7Z Approved [56]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine D1 receptor (D1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenyltoloxamine DMKAEQW Allergy 4A80-4A85 Approved [57]
Pergolide DM14MAE Parkinson disease 8A00.0 Approved [5]
Methylergonovine DMBEX4O Spontaneous abortion JA00.0 Approved [58]
Fenoldopam DMFAOKP Hypertension BA00-BA04 Approved [59]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [60]
Ecopipam DMS9R43 Cocaine addiction 6C45.2 Phase 3 [61]
DAS-431 DMM3BPL Dementia 6D80-6D86 Phase 2 [62]
Dihydrexidine DMACPQO Psychotic disorder 6A20-6A25 Phase 1/2 [63]
Lu AF28996 DMY572G Parkinson disease 8A00.0 Phase 1 [64]
BAM-1110 DMPMKUF Parkinson disease 8A00.0 Discontinued in Phase 2 [65]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [5]
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [11]
Macitentan DMP79A1 Cardiovascular disease BA00-BE2Z Approved [4]
Sparsentan DMMP51W IgA nephropathy MF8Y Approved [66]
LU302146 DMMJVXZ Pulmonary hypertension BB01 Approved [67]
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [68]
Clazosentan DMQSBX4 Cerebral vasospasm BA85.Z Phase 3 [69]
PF-1228305 DMS1EQ7 Pulmonary hypertension BB01 Phase 3 [70]
Darusentan DMN8DQH Hypotension BA20-BA21 Phase 3 [71]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [72]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [49]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [50]
Fluoxetine DM3PD2C Bipolar depression Approved [5]
Vortioxetine DM6F1PU Major depressive disorder 6A70.3 Approved [4]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [73]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [52]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [53]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [5]
Nortriptyline DM4KDYJ Depression 6A70-6A7Z Approved [5]
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [5]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [40]
Fesoterodine fumarate DM13495 Overactive bladder GC50.0 Approved [74]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [75]
Clidinium DMUMQZ0 Abdominal stomach pain DD91.4 Approved [76]
Trihexyphenidyl DMB19L8 Dystonia 8A02 Approved [77]
Oxyphenonium DMMQHOZ Visceral spasms MD81.4 Approved [78]
Benztropine DMGZOVN Parkinson disease 8A00.0 Approved [79]
Glycopyrrolate DM2M3ZA Anaesthesia 9A78.6 Approved [80]
Pirenzepine DMP6M1N Peptic ulcer DA61 Approved [81]
Cycrimine DM8C43Q Parkinson disease 8A00.0 Approved [82]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methamphetamine DMPM4SK Anxiety Approved [83]
Propericiazine DME9JNL Psychiatric disorder 6E8Z Approved [84]
Methoxamine DMF5XQH Hypertension BA00-BA04 Approved [85]
Phendimetrazine DM6TS1N Obesity 5B81 Approved [86]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [36]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [87]
Sunepitron DM6M8ZX N. A. N. A. Discontinued in Phase 3 [88]
MAZAPERTINE DMRHYAU N. A. N. A. Discontinued in Phase 2 [37]
SOU-001 DMPAEK5 Urinary incontinence MF50.2 Discontinued in Phase 2 [89]
SNAP-5089 DMROJEN Heart arrhythmia BC65 Terminated [90]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Acetylcholinesterase (AChE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [91]
Donepezil DMIYG7Z Advanced cancer 2A00-2F9Z Approved [92]
Malathion DMXZ84M Pediculus capitis infestation 1G00.0 Approved [93]
Galantamine DMEO794 Alzheimer disease 8A20 Approved [94]
Huperzine A DMMAWLU Alzheimer disease 8A20 Approved [95]
Neostigmine DM6T2J3 Myasthenia gravis 8C6Y Approved [96]
YM443 DMNZCI1 Functional dyspepsia DD90.3 Approved [74]
Ambenonium DMOP0BL Myasthenia gravis 8C6Y Approved [97]
Demecarium bromide DMAYEU1 Open-angle glaucoma 9C61 Approved [98]
Isoflurophate DMBSK7X Glaucoma/ocular hypertension 9C61 Approved [99]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Vamorolone DM047HI Duchenne muscular dystrophy 8C70.1 Approved [100]
CORT125281 DMHBOUX Prostate cancer 2C82.0 Phase 2 [9]
ISIS-GCCR DMICMNU Diabetic complication 5A2Y Phase 2 [101]
ORIC-101 DMR12S0 Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
AZD9567 DMAXHC0 Rheumatoid arthritis FA20 Phase 1 [100]
A-348441 DM25CBW Type-2 diabetes 5A11 Phase 1 [102]
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE DMTPQ84 Discovery agent N.A. Investigative [103]
deoxycorticosterone DMW6YLS Discovery agent N.A. Investigative [103]
LGD-5552 DM67KWM Discovery agent N.A. Investigative [104]
AL-43 DMLEDHR Discovery agent N.A. Investigative [105]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Histamine H2 receptor (H2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [106]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [107]
Famotidine DMRL3AB Gastric ulcer DA60 Approved [107]
Nizatidine DMGFV3Z Acid-reflux disorder DA22 Approved [108]
Betazole DMUFGAY Gastric secretory disorder DD90 Approved [109]
Ebrotidine DMV5KR3 Duodenal ulcer DA63 Withdrawn from market [110]
Pibutidine DMXSTRM Ulcerative colitis DD71 Discontinued in Phase 3 [111]
Osutidine DMN7TL8 Duodenal ulcer DA63 Discontinued in Phase 3 [112]
KU-1257 DMZMFX6 Duodenal ulcer DA63 Discontinued in Phase 3 [113]
Lavoltidine DMTY5VE Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [114]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2B receptor (HTR2B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [115]
Triflupromazine DMKFQJP Nausea MD90 Approved [116]
Minaprine DM0EP7M Depression 6A70-6A7Z Approved [117]
SPN-812 DMTV7XH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [118]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [119]
PRX-08066 DMR7H2V Pulmonary arterial hypertension BB01.0 Phase 2 [120]
Pyrimidine derivative 29 DMVOYJ8 N. A. N. A. Patented [121]
Pyrimidine derivative 26 DM90WKN N. A. N. A. Patented [121]
Pyrimidine derivative 23 DM5MLQU N. A. N. A. Patented [121]
Pyrimidine derivative 25 DM51MFS N. A. N. A. Patented [121]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2A receptor (HTR2A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [115]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [122]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [123]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [4]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [124]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [125]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [126]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [127]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [128]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [60]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
IB-MECA DM9G5XD Psoriasis vulgaris EA90 Phase 3 [129]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [130]
NITD609 DMQHBSX Malaria 1F40-1F45 Phase 2 [131]
CF102 DMP56WJ Hepatocellular carcinoma 2C12.02 Phase 2 [132]
SCH-442416 DMQ2K1V N. A. N. A. Phase 1 [133]
AST-004 DM5WMG7 Stroke 8B20 Phase 1 [134]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [135]
BAY 60-6583 DMTEJV1 Myocardial ischemia BA6Z Preclinical [136]
CF602 DM0ULO2 Inflammation 1A00-CA43.1 Preclinical [132]
CF502 DMQSJ20 Inflammation 1A00-CA43.1 Preclinical [132]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Propranolol DM79NTF Angina pectoris BA40 Approved [137]
Epinephrine DM3KJBC Acute asthma CA23 Approved [138]
Norepinephrine DMOUC09 Alopecia ED70 Approved [139]
Atenolol DMNKG1Z Angina pectoris BA40 Approved [140]
Acebutolol DM0TI4U Hypertension BA00-BA04 Approved [140]
Metoprolol DMOJ0V6 Acute coronary syndrome BA41 Approved [140]
Timolol DM3NXRU High blood pressure BA00 Approved [141]
Isoproterenol DMK7MEY Atrioventricular block Approved [142]
Betaxolol DM6EUL5 Hypertension BA00-BA04 Approved [143]
Sotalol DML60TN Sinus rhythm disorder BC9Y Approved [144]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [40]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [41]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [75]
Methylscopolamine DM5VWOB Peptic ulcer DA61 Approved [145]
Gallamine Triethiodide DMPO0MS Stabilize muscle contraction FB3Z Approved [146]
FP-1097 DMC1F2T Urinary incontinence MF50.2 Phase 2 [147]
PSD-506 DMT0KB1 Overactive bladder GC50.0 Discontinued in Phase 2 [148]
Otenzepad DMRXHAC Heart failure BD10-BD13 Discontinued in Phase 2 [149]
SCH-211803 DM92E0W Parkinson disease 8A00.0 Discontinued in Phase 1 [150]
Alvameline DMLN0Y5 Alzheimer disease 8A20 Terminated [151]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aprepitant DM053KT Depression 6A70-6A7Z Approved [152]
Selegiline DM6034S Major depressive disorder 6A70.3 Approved [11]
Rolapitant DM8XP26 Chemotherapy-induced nausea MD90 Approved [153]
Netupitant DMEKAYI Chemotherapy-induced nausea MD90 Phase 3 [153]
Serlopitant DM5VH6U Prurigo nodularis EC91.0 Phase 3 [154]
LY-686017 DM7WORZ Atopic dermatitis EA80 Phase 3 [155]
Elinzanetant DMC6EFI Hot flushes GA30 Phase 3 [156]
CP-122721 DMSWLM5 Major depressive disorder 6A70.3 Phase 2 [157]
FR139317 DMEL5SV Hypertension BA00-BA04 Phase 2 [11]
VOFOPITANT HYDROCHLORIDE DMQMYP5 Vomiting MD90 Phase 2 [158]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Opioid receptor mu (MOP)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [159]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [160]
Hydromorphone DMHP21E Back pain ME84.Z Approved [161]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [54]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [162]
Alfentanil DMVO0UB Anaesthesia 9A78.6 Approved [163]
Naloxegol DML0B41 Opioid-induced constipation DB32.1 Approved [164]
Eluxadoline DMYZ0P1 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [165]
Nalfurafine hcl DMA9DHW Uremic pruritus EC90.10 Approved [166]
Oxycodone DMXLKHV Osteoarthritis FA00-FA05 Approved [167]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ibodutant DMT67EH Irritable bowel syndrome DD91.0 Phase 3 [168]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [169]
Rambazole DMP2DNS Psoriasis vulgaris EA90 Phase 2 [170]
Nepadutant DMPMF6L Infantile colics DD93.1 Phase 1/2 [171]
Saredutant DMSRJY3 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [172]
CS-003 DM1AEVT Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [173]
FK-224 DM1JUS0 Asthma CA23 Discontinued in Phase 2 [174]
DNK-333 DM4ZO01 Irritable bowel syndrome DD91.0 Discontinued in Phase 2 [175]
AVE-5883 DM3P84V Asthma CA23 Discontinued in Phase 1/2 [176]
UK-224671 DMDTRJB Urinary incontinence MF50.2 Discontinued in Phase 1 [177]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxazosin DM9PLRH Benign prostatic hyperplasia GA90 Approved [178]
Armodafinil DMGB035 Malignant glioma 2A00.0 Approved [179]
Alfuzosin DMZVMKF Benign prostatic hyperplasia GA90 Approved [180]
Moxisylyte DMFCLYW Erectile dysfunction HA01.1 Approved [181]
Terazosin DM3JCVS Benign prostatic hyperplasia GA90 Approved [182]
Bunazosin DM4I8O7 Glaucoma/ocular hypertension 9C61 Approved [183]
Trimazosin DM1QLST Congestive heart failure BD10 Approved [184]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [36]
DL-017 DMM8GZT Hypertension BA00-BA04 Phase 1 [185]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [186]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine transporter (DAT)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [52]
Dasotraline DMLDQFV Attention deficit hyperactivity disorder 6A05.Z Approved [187]
Methylphenidate DM7SJD6 Attention deficit hyperactivity disorder 6A05.Z Approved [188]
Modafinil DMYILBE Malignant glioma 2A00.0 Approved [5]
Phenmetrazine DMXYTN9 Obesity 5B81 Approved [189]
Ioflupane i-123 DMNARJT Parkinson disease 8A00.0 Approved [74]
DEXMETHYLPHENIDATE HYDROCHLORIDE DM8WBAH Attention deficit hyperactivity disorder 6A05.Z Approved [190]
Altropane DMO9WDS Attention deficit hyperactivity disorder 6A05.Z Approved [191]
Amitifadine DMS1X67 Obesity 5B81 Phase 3 [192]
NAV5001 DMRSI1M Dementia 6D80-6D86 Phase 3 [191]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 4 receptor (HTR4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisapride DMY7PED Gastroesophageal reflux disease DA22.Z Approved [193]
Tegaserod DM3XYD1 Irritable bowel syndrome DD91.0 Approved [194]
R0-93877 DMM4U9G Constipation DD91.1 Approved [195]
HTF 919 DM78G6F Constipation DD91.1 Approved [196]
Mosapride DM2VOQ3 N. A. N. A. Phase 4 [197]
Renzapride DM7HQNX Irritable bowel syndrome DD91.0 Phase 3 [198]
Lintopride DMSHGWN Nausea MD90 Phase 2 [199]
TD-8954 DM3C9NV Gastrointestinal disease DE2Z Phase 2 [200]
SB-207266A DM27KFY Irritable bowel syndrome DD91.0 Phase 2 [195]
YKP-GI DM740LV Constipation DD91.1 Phase 2 [201]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 3A receptor (HTR3A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dolasetron DMMG26Z Nausea MD90 Approved [202]
Alosetron DML2A03 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [203]
Tropisetron DMNSJ7V Fibromyalgia MG30.01 Approved [204]
Palonosetron DMBHMOX Nausea MD90 Approved [205]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [204]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [206]
Cilansetron DMP0NGX Irritable bowel syndrome DD91.0 Phase 3 [207]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [208]
Norcisapride DMJSKUI Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [209]
YM-114 DML2IXO Nausea MD90 Discontinued in Phase 2 [210]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Histamine H3 receptor (H3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pitolisant DM8RFNJ Excessive daytime sleepiness MG42 Approved [211]
SUVN-G3031 DM3BO8G Cognitive impairment 6D71 Phase 3 [212]
JNJ-17216498 DM1GRCU Narcolepsy 7A20 Phase 2 [213]
GSK239512 DMBJMZC Alzheimer disease 8A20 Phase 2 [11]
JNJ-39220675 DM0WY3H Alcohol dependence 6C40.2 Phase 2 [214]
AZD-5213 DMOZ04X Alzheimer disease 8A20 Phase 2 [215]
Bavisant DM6CVZ5 Attention deficit hyperactivity disorder 6A05.Z Phase 2 [216]
ABT-288 DM7X54F Alzheimer disease 8A20 Phase 2 [217]
SAR-110894 DMCLEXM Alzheimer disease 8A20 Phase 2 [215]
ABT-652 DMLEO2Z Diabetic neuropathy 8C0Z Phase 2 [218]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [219]
Haloperidol DM96SE0 Delirium Approved [220]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [221]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [222]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [223]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [224]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [225]
Pimozide DMW83TP Schizophrenia 6A20 Approved [226]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [227]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [123]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tolterodine DMSHPW8 Overactive bladder GC50.0 Approved [228]
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [40]
Tiotropium DMFDC0Q Chronic obstructive pulmonary disease CA22 Approved [229]
Ipratropium DMFQ320 Obstructive lung disease CA22.Z Approved [230]
Darifenacin DMWXLYZ Overactive bladder GC50.0 Approved [231]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [232]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [75]
Solifenacin DMG592Q Overactive bladder GC50.0 Approved [233]
Methylscopolamine DM5VWOB Peptic ulcer DA61 Approved [234]
Cevimeline DMWSMND Sjogren syndrome 4A43.20 Approved [235]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trimethaphan DMHF4IQ Aneurysm BD51.Z Approved [236]
Pentolinium DM38VYQ Hypotension BA20-BA21 Approved [237]
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [238]
ABT-594 DMGMBCW N. A. N. A. Discontinued in Phase 2 [239]
ABT-418 DMNP72I Alzheimer disease 8A20 Discontinued in Phase 2 [240]
HOMOEPIBATIDINE DMHP9WV N. A. N. A. Terminated [238]
Barbituric acid derivative DM2I19P Discovery agent N.A. Investigative [241]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol DMDUGZS Discovery agent N.A. Investigative [242]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol DMDUI8R Discovery agent N.A. Investigative [242]
BOLDINE DMMVB5P Discovery agent N.A. Investigative [243]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methylnaltrexone bromide DMZTGN2 Opioid-induced constipation DB32.1 Approved [244]
Bremelanotide DM20LIM Hypoactive sexual desire dysfunction HA00 Approved [245]
Setmelanotide DMPVRN9 Obesity 5B81 Approved [246]
Amylin DMWDEN0 N. A. N. A. Phase 4 [247]
AMG 386 DMQJXL4 Breast cancer 2C60-2C65 Phase 3 [244]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [169]
PF-446687 DML38VU Female sexual arousal dysfunction HA01.1 Phase 2 [248]
AP-1030 DMBGA35 Metabolic disorder 5C50-5D2Z Phase 1/2 [148]
PF-07258669 DM3CJ5N Malnutrition 5B50-5B71 Phase 1 [249]
PT-14 DMYM9JL Erectile dysfunction HA01.1 Discontinued in Phase 2 [250]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [251]
NABILONE DMVRYT2 Insomnia 7A00-7A0Z Approved [252]
Orlistat DMRJSP8 Obesity 5B81 Approved [253]
SR141716A DMCO5JZ Obesity 5B81 Approved [254]
Tebipenem DMVSX6O Urinary tract infection GC08 Phase 3 [244]
Conatumumab DM2UOSN Colorectal cancer 2B91.Z Phase 2 [255]
GW-42004 DMY3KSU Lipid metabolism disorder 5C52.Z Phase 2 [256]
SR-147778 DMNAECP Obesity 5B81 Phase 2 [257]
Nimacimab DM21Z68 Diabetic nephropathy GB61.Z Phase 2 [258]
AEF0117 DMQ1GH4 Marijuana use disorder 6C41 Phase 2 [259]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Caffeine DMKBJWP Allergic rhinitis CA08.0 Approved [260]
Istradefylline DM20VSK Parkinson disease 8A00.0 Approved [261]
Regadenoson DM76VHG Radionuclide imaging N.A. Approved [74]
Tozadenant DMATC14 Parkinson disease 8A00.0 Phase 3 [262]
Binodenoson DMVHF8G Hypertension BA00-BA04 Phase 3 [263]
Apadenoson DMD8QTC Coronary artery disease BA80 Phase 3 [264]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [130]
Dexefaroxan DMTY4KN Parkinson disease 8A00.0 Phase 2 [265]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [266]
BIIB014 DMH7RJ1 Parkinson disease 8A00.0 Phase 2 [267]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [268]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [269]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [270]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [271]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [272]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [270]
Doxepin DMPI98T Anxiety Approved [273]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [270]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [274]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [275]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [5]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [276]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [277]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [278]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [4]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [279]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [280]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [281]
Treximet DMU54QB Migraine 8A80 Approved [11]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [6]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 7 receptor (HTR7)
Drug Name Drug ID Indication ICD 11 Highest Status REF
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [8]
JNJ-18038683 DMV1T59 Major depressive disorder 6A70.3 Phase 2 [282]
AVN-101 DMOGFNI Cognitive impairment 6D71 Phase 2 [283]
ATI-9242 DM6GKMU Schizophrenia 6A20 Phase 1 [284]
PMID30124346-Compound-34TABLE4 DM2G3VE Attention deficit hyperactivity disorder 6A05.Z Patented [186]
PMID30124346-Compound-13TABLE4 DMHTJVA Attention deficit hyperactivity disorder 6A05.Z Patented [186]
Carbamide derivative 2 DMW5GI3 N. A. N. A. Patented [285]
4-oxadiazole derivative 1 DMWFHKR N. A. N. A. Patented [285]
SB-269970 DM8WTGA Sleep-wake disorder 7A00-7B2Z Terminated [286]
(+/-)-nantenine DM0L3GE Discovery agent N.A. Investigative [287]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Promazine DMZAL7W Acute intermittent hepatic porphyria 5C58.11 Approved [288]
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [40]
Pilocarpine DMV9ADG Glaucoma/ocular hypertension 9C61 Approved [289]
Anisodine DMNOSWU Central and peripheral nervous disease 8A04-8E7Z Approved [290]
Atropine DMEN6X7 Organophosphate poisoning NE6Z Approved [291]
Propiverine DMUWBIJ Urinary incontinence MF50.2 Approved [292]
Umeclidinium DM4E8O9 Chronic obstructive pulmonary disease CA22 Approved [293]
Cimetropium bromide DMZHPNE Gastric motility disorder DA21 Approved [294]
Butylscopolamine DMZKXB7 Dysmenorrhea GA34.3 Approved [295]
Trospium DMX6RTG Overactive bladder GC50.0 Approved [86]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [238]
TC-5214 DM8AM60 Palmar hyperhidrosis EE00.00 Phase 2 [154]
SUVN-911 DMLPBVF Major depressive disorder 6A70.3 Phase 1 [8]
AZD-9684 DMHA5ME Thrombosis DB61-GB90 Discontinued in Phase 2 [296]
ABT-594 DMGMBCW N. A. N. A. Discontinued in Phase 2 [239]
ABT-418 DMNP72I Alzheimer disease 8A20 Discontinued in Phase 2 [297]
HOMOEPIBATIDINE DMHP9WV N. A. N. A. Terminated [238]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol DMDUGZS Discovery agent N.A. Investigative [242]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol DMDUI8R Discovery agent N.A. Investigative [242]
BOLDINE DMMVB5P Discovery agent N.A. Investigative [243]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 2C receptor (HTR2C)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [115]
Lorcaserin DMG6OYJ Obesity 5B81 Approved [254]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [298]
Mirtazapine DML53ZJ Depression 6A70-6A7Z Approved [299]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [300]
Methysergide DM1EF73 Migraine 8A80 Approved [301]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [302]
M100907 DM7ZFBA Sleep-wake disorder 7A00-7B2Z Phase 3 [303]
SR46349B DM1ODMR Primary insomnia 7A00 Phase 3 [304]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [119]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
NEUROPEPTIDE-Y DMINQP1 N. A. N. A. Phase 2 [305]
H-409/22 DMYJ9CF Cardiovascular disease BA00-BE2Z Discontinued in Phase 2 [306]
PD-160170 DMB9Z4C Heart disease BA41-BA42 Preclinical [244]
GI-264879A DM25N8B Obesity 5B81 Preclinical [244]
SR 120819A DMETDFM Eating disorder 6B82 Terminated [307]
BIBP 3226 DMYBR9D Hypertension BA00-BA04 Terminated [308]
H-[Trp-Arg-Nva-Arg-Tyr]3-NH2 DMKH8PF Discovery agent N.A. Investigative [309]
Sub[-Trp-Arg-Nva-Arg-Tyr-NH2]2 DM4SWQA Discovery agent N.A. Investigative [309]
Pim[-Trp-Arg-Nva-Arg-Tyr-NH2]2 DMBERSG Discovery agent N.A. Investigative [309]
Sub[-Tyr-Arg-Leu-Arg-Tyr-NH2]2 DM56MOV Discovery agent N.A. Investigative [309]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Caffeine DMKBJWP Allergic rhinitis CA08.0 Approved [260]
Rolofylline DMSZPR3 Heart failure BD10-BD13 Phase 3 [310]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [130]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [266]
SELODENOSON DMQM3IX Cardiac arrhythmias BC9Z Phase 2 [311]
Apaxifylline DMQMV9F Cognitive impairment 6D71 Phase 2 [312]
SLV320 DM867BJ Heart failure BD10-BD13 Phase 2 [313]
DTI-0009 DMV84OK Atrial fibrillation BC81.3 Phase 2 [311]
Capadenoson DMYWO62 Atrial fibrillation BC81.3 Phase 2 [314]
BAY 1067197 DM4JGNH Heart failure BD10-BD13 Phase 2 [315]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
SILODOSIN DMJSBT6 Benign prostatic hyperplasia GA90 Approved [316]
NAFTOPIDIL DMQ8R4E Hypertension BA00-BA04 Approved [316]
Tamsulosin DM5QF9V Benign prostatic hyperplasia GA90 Approved [5]
Xatral DMLHOA0 Benign prostatic hyperplasia GA90 Approved [317]
Dutasteride + tamsulosin DM6P8HU Benign prostatic hyperplasia GA90 Phase 3 [11]
Besipirdine DMLVNTA Cognitive impairment 6D71 Phase 3 [318]
MEDETOMIDINE DMX9Y7V Pain MG30-MG3Z Phase 2 [36]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [186]
PMID30124346-Compound-LDT66 DMJMTNL Benign prostatic hyperplasia GA90 Patented [186]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [87]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Melatonin DMKWFBT Depression 6A70-6A7Z Approved [319]
Ramelteon DM7IW9J Insomnia 7A00-7A0Z Approved [320]
Tasimelteon DMLOQ1V Insomnia 7A00-7A0Z Approved [321]
Neu-P11 DMIQDFW Alzheimer disease 8A20 Phase 2 [322]
LY-156735 DM5IX9M Anxiety disorder 6B00-6B0Z Phase 2 [323]
Agomelatine DMXYA5K Major depressive disorder 6A70.3 Withdrawn from market [324]
Luzindole DMXRJQV Sleep-wake disorder 7A00-7B2Z Terminated [325]
S-20928 DMQDWMJ Sleep-wake disorder 7A00-7B2Z Terminated [326]
GR-133347 DMNRJA0 Anxiety disorder 6B00-6B0Z Terminated [327]
GR-131663 DMKAGLV Anxiety disorder 6B00-6B0Z Terminated [328]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Inhibitor [2]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Inhibitor [2]
5-HT 2B receptor (HTR2B) TT0K1SC 5HT2B_HUMAN Inhibitor [2]
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Inhibitor [2]
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Inhibitor [2]
5-HT 4 receptor (HTR4) TT07C3Y 5HT4R_HUMAN Inhibitor [2]
5-HT 7 receptor (HTR7) TTO9X1H 5HT7R_HUMAN Inhibitor [2]
Acetylcholinesterase (AChE) TT1RS9F ACES_HUMAN Inhibitor [2]
Adenosine A1 receptor (ADORA1) TTK25J1 AA1R_HUMAN Inhibitor [2]
Adenosine A2a receptor (ADORA2A) TTM2AOE AA2AR_HUMAN Inhibitor [2]
Adenosine A3 receptor (ADORA3) TTJFY5U AA3R_HUMAN Inhibitor [2]
Adrenergic receptor alpha-1A (ADRA1A) TTNGILX ADA1A_HUMAN Inhibitor [2]
Adrenergic receptor alpha-1B (ADRA1B) TTBRKXS ADA1B_HUMAN Inhibitor [2]
Adrenergic receptor alpha-1D (ADRA1D) TT34BHT ADA1D_HUMAN Inhibitor [2]
Adrenergic receptor alpha-2A (ADRA2A) TTWG9A4 ADA2A_HUMAN Inhibitor [2]
Adrenergic receptor beta-1 (ADRB1) TTR6W5O ADRB1_HUMAN Inhibitor [2]
Cannabinoid receptor 1 (CB1) TT6OEDT CNR1_HUMAN Inhibitor [2]
Dopamine D1 receptor (D1R) TTZFYLI DRD1_HUMAN Inhibitor [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Inhibitor [2]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Inhibitor [2]
Dopamine transporter (DAT) TTVBI8W SC6A3_HUMAN Inhibitor [2]
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Inhibitor [2]
Gastrin/cholecystokinin type B receptor (CCKBR) TTVFO0U GASR_HUMAN Inhibitor [2]
Glucocorticoid receptor messenger RNA (GCR mRNA) TTOZRK6 GCR_HUMAN Inhibitor [2]
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Inhibitor [2]
Histamine H2 receptor (H2R) TTQHJ1K HRH2_HUMAN Inhibitor [2]
Histamine H3 receptor (H3R) TT9JNIC HRH3_HUMAN Inhibitor [2]
Melanocortin receptor 4 (MC4R) TTD0CIQ MC4R_HUMAN Inhibitor [2]
Melatonin receptor type 1A (MTNR1A) TT0WAIE MTR1A_HUMAN Inhibitor [2]
Muscarinic acetylcholine receptor M1 (CHRM1) TTZ9SOR ACM1_HUMAN Inhibitor [3]
Muscarinic acetylcholine receptor M2 (CHRM2) TTYEG6Q ACM2_HUMAN Inhibitor [2]
Muscarinic acetylcholine receptor M3 (CHRM3) TTQ13Z5 ACM3_HUMAN Inhibitor [2]
Muscarinic acetylcholine receptor M4 (CHRM4) TTQ3JTF ACM4_HUMAN Inhibitor [2]
Muscarinic acetylcholine receptor M5 (CHRM5) TTH18TF ACM5_HUMAN Inhibitor [2]
Neuronal acetylcholine receptor alpha-4 (CHRNA4) TT4H1MQ ACHA4_HUMAN Inhibitor [2]
Neuronal acetylcholine receptor beta-2 (CHRNB2) TT5KPZR ACHB2_HUMAN Inhibitor [2]
Neuropeptide Y receptor type 1 (NPY1R) TTRK9JT NPY1R_HUMAN Inhibitor [2]
Neurotensin receptor type 1 (NTSR1) TTTUMEP NTR1_HUMAN Inhibitor [2]
Norepinephrine transporter (NET) TTAWNKZ SC6A2_HUMAN Inhibitor [2]
Opioid receptor mu (MOP) TTKWM86 OPRM_HUMAN Inhibitor [2]
Serotonin transporter (SERT) TT3ROYC SC6A4_HUMAN Inhibitor [2]
Substance-K receptor (TACR2) TTYO0A3 NK2R_HUMAN Inhibitor [2]
Substance-P receptor (TACR1) TTZPO1L NK1R_HUMAN Inhibitor [2]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 289).
2 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
3 Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists. Eur J Pharmacol. 2009 Mar 1;605(1-3):53-6.
4 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
7 Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
10 Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D 2 /D 3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants. Clin Pharmacol Drug Dev. 2021 Jan 18.
11 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
12 Neurotensin inversely modulates maternal aggression. Neuroscience. 2009 Feb 18;158(4):1215-23.
13 Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic. J Med Chem. 2010 Jun 24;53(12):4623-32.
14 Clinical status of anti-cancer agents derived from marine sources. Anticancer Agents Med Chem. 2008 Aug;8(6):603-17.
15 Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2. Mol Pharmacol. 2001 Dec;60(6):1392-8.
16 Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy. J Med Chem. 2009 Apr 9;52(7):1803-13.
17 Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus. Mol Pharmacol. 2003 Aug;64(2):421-9.
18 [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor. Mol Pharmacol. 1995 May;47(5):1050-6.
19 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 309).
20 Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensi... Bioorg Med Chem. 2008 Oct 15;16(20):9359-68.
21 Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
22 Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
23 Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
24 Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
25 Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
26 The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
27 Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
28 Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
29 CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
30 Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.
31 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
32 Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5.
33 alpha2A-adrenergic receptors heterosynaptically regulate glutamatergic transmission in the bed nucleus of the stria terminalis. Neuroscience. 2009 Sep 29;163(1):339-51.
34 Scientific rationale for the use of alpha2A-adrenoceptor agonists in treating neuroinflammatory cognitive disorders. Mol Psychiatry. 2023 Apr 7:1-13.
35 Clinical pipeline report, company report or official report of Klus Pharma
36 A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
37 A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.
38 Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges. Cardiovasc Hematol Agents Med Chem. 2009 October; 7(4): 260-269.
39 Design and synthesis of novel dihydropyridine alpha-1a antagonists. Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.
40 Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. J Med Chem. 1993 Apr 2;36(7):842-7.
41 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. J Med Chem. 1998 Jun 4;41(12):2047-55.
42 The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 rec... Psychopharmacology (Berl). 2007 Oct;194(3):347-59.
43 Diphenidol-related diamines as novel muscarinic M4 receptor antagonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2972-6.
44 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
45 Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. J Med Chem. 1990 Feb;33(2):809-14.
46 Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. J Med Chem. 1989 Dec;32(12):2573-82.
47 Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6.
48 Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. J Nat Prod. 2005 Jul;68(7):1061-5.
49 Augmentation effect of combination therapy of aripiprazole and antidepressants on forced swimming test in mice. Psychopharmacology (Berl). 2009 Sep;206(1):97-107.
50 Treatment of comorbid pain with serotonin norepinephrine reuptake inhibitors. CNS Spectr. 2008 Jul;13(7 Suppl 11):22-6.
51 Invivo antioxidant status: a putative target of antidepressant action. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Mar 17;33(2):220-8.
52 Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81.
53 Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
54 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
55 Antidepressants suppress production of the Th1 cytokine interferon-gamma, independent of monoamine transporter blockade. Eur Neuropsychopharmacol. 2006 Oct;16(7):481-90.
56 Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42.
57 Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.
58 Reinforcement in an in vitro analog of appetitive classical conditioning of feeding behavior in Aplysia: blockade by a dopamine antagonist. Learn Mem. 2005 May-Jun;12(3):216-20.
59 Etiology of iodinated radiocontrast nephrotoxicity and its attenuation by beraprost. Yakugaku Zasshi. 2008 Jul;128(7):1023-9.
60 Clinical pipeline report, company report or official report of Lundbeck.
61 A D1 receptor antagonist, ecopipam, for treatment of tics in Tourette syndrome.Clin Neuropharmacol.2014 Jan-Feb;37(1):26-30.
62 Adrogolide HCl (ABT-431; DAS-431), a prodrug of the dopamine D1 receptor agonist, A-86929: preclinical pharmacology and clinical data. CNS Drug Rev. 2001 Fall;7(3):305-16.
63 trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization o... J Med Chem. 2006 Nov 16;49(23):6848-57.
64 Clinical pipeline report, company report or official report of Lundbeck
65 Therapeutic effects of dopamine D1/D2 receptor agonists on detrusor hyperreflexia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned parkinso... J Pharmacol Exp Ther. 1998 Jul;286(1):228-33.
66 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
67 Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
68 Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
69 Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subar... Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918.
70 Pfizer. Product Development Pipeline. March 31 2009.
71 Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
72 Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.
73 Psychopharmacological treatment of dermatological patients--when simply talking does not help. J Dtsch Dermatol Ges. 2007 Dec;5(12):1101-6.
74 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
75 Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
76 Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
77 The role of M1 muscarinic cholinergic receptors in the discriminative stimulus properties of N-desmethylclozapine and the atypical antipsychotic dr... Psychopharmacology (Berl). 2009 Apr;203(2):295-301.
78 Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
79 Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60.
80 Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701.
81 Negative crosstalk between M1 and M2 muscarinic autoreceptors involves endogenous adenosine activating A1 receptors at the rat motor endplate. Neurosci Lett. 2009 Aug 14;459(3):127-31.
82 Capillary gas chromatography of trihexyphenidyl, procyclidine and cycrimine in biological fluids. J Chromatogr. 1989 Sep 29;494:135-42.
83 Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9.
84 Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91.
85 Activation of alpha1-adrenoceptors inhibits growth hormone secretion in humans. Exp Clin Endocrinol Diabetes. 2009 Oct;117(9):460-2.
86 Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
87 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
88 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment o... J Med Chem. 2006 Jun 1;49(11):3116-35.
89 Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
90 Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716.
91 Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19.
92 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2465).
93 Acetylcholinesterase activity in Corbicula fluminea Mull., as a biomarker of organophosphate pesticide pollution in Pinacanauan River, Philippines. Environ Monit Assess. 2010 Jun;165(1-4):331-40.
94 [From symptomatic to disease modifying therapy Recent developments in the pharmacotherapy of Alzheimer's disease]. Fortschr Neurol Psychiatr. 2009 Jun;77(6):326-33.
95 Huperzine A attenuates cognitive deficits and brain injury in neonatal rats after hypoxia-ischemia. Brain Res. 2002 Sep 13;949(1-2):162-70.
96 Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet. J Sep Sci. 2009 May;32(10):1748-56.
97 Alpha6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology. 2008 Aug;33(9):2158-66.
98 The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs. Vet Ophthalmol. 2003 Mar;6(1):23-5.
99 Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem Biol. 2003 Jun;10(6):491-502.
100 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
101 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011).
102 Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90.
103 Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding. J Biol Chem. 2000Jun 23;275(25):19041-9.
104 Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9.
105 Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.
106 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
107 Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
108 Does the use of nizatidine, as a pro-kinetic agent, improve gastric emptying in patients post-oesophagectomy J Gastrointest Surg. 2009 Mar;13(3):432-7.
109 Effect of nizatidine and cimetidine on betazole-stimulated gastric secretion of normal subjects: comparison of effects on acid, water, and pepsin. Am J Gastroenterol. 1988 Jan;83(1):32-6.
110 Histamine H2-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.
111 Comparative pharmacology of epibatidine: a potent agonist for neuronal nicotinic acetylcholine receptors. Mol Pharmacol. 1995 Oct;48(4):774-82.
112 Effects of osutidine (T-593) and its enantiomers on gastric mucosal hemodynamics and mucosal integrity in anesthetized rats. Arzneimittelforschung. 2001 Jan;51(1):46-50.
113 Pharmacological profiles of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy] propyl] urea. Arzneimittelforschung. 1993 Feb;43(2):129-33.
114 New and Future Drug Development for Gastroesophageal Reflux Disease. J Neurogastroenterol Motil. 2014 January; 20(1): 6-16.
115 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
116 Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
117 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
118 New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
119 Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
120 Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
121 Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
122 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
123 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
124 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
125 Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.
126 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
127 Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
128 Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
129 A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.
130 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
131 Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.
132 2011 Pipeline of Can-Fite BioPharm.
133 Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4.
134 Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke. Stroke. 2022 Jan;53(1):238-248.
135 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
136 Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.
137 Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8.
138 Adrenergic activation of electrogenic K+ secretion in guinea pig distal colonic epithelium: involvement of beta1- and beta2-adrenergic receptors. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G269-77.
139 Impact of exogenous beta-adrenergic receptor stimulation on hepatosplanchnic oxygen kinetics and metabolic activity in septic shock. Crit Care Med. 1999 Feb;27(2):325-31.
140 Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6.
141 Topical dorzolamide 2%/timolol 0.5% ophthalmic solution: a review of its use in the treatment of glaucoma and ocular hypertension. Drugs Aging. 2006;23(12):977-95.
142 Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404.
143 beta-adrenergic enhancement of brain kynurenic acid production mediated via cAMP-related protein kinase A signaling. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Apr 30;33(3):519-29.
144 beta(2)-adrenoceptors are critical for antidepressant treatment of neuropathic pain. Ann Neurol. 2009 Feb;65(2):218-25.
145 Methylacridinium and its cholinergic properties. Neurotox Res. 2009 Nov;16(4):372-7.
146 Cholinergic regulation of the corpora allata in adult male loreyi leafworm Mythimna loreyi. Arch Insect Biochem Physiol. 2002 Apr;49(4):215-24.
147 Clinical pipeline report, company report or official report of FemmePharma.
148 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
149 Beneficial effect of muscarinic-2 antagonist on dilated cardiomyopathy induced by autoimmune mechanism against muscarinic-2 receptor. J Cardiovasc Pharmacol. 2001 Oct;38 Suppl 1:S43-9.
150 Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists. J Med Chem. 2002 Dec 5;45(25):5415-8.
151 In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro. Psychopharmacology (Berl). 1998 Jun;137(3):233-40.
152 Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
153 Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
154 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
155 Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
156 Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
157 A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
158 Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.
159 Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8.
160 Antianalgesia: stereoselective action of dextro-morphine over levo-morphine on glia in the mouse spinal cord.J Pharmacol Exp Ther.2005 Sep;314(3):1101-8.
161 Clinical pipeline report, company report or official report of signaturerx.
162 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
163 Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87.
164 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
165 Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.Biochem Pharmacol.2014 Dec 1;92(3):448-56.
166 Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
167 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 319).
168 Antagonist profile of ibodutant at the tachykinin NK2 receptor in guinea pig isolated bronchi. Eur J Pharmacol. 2013 Nov 15;720(1-3):180-5.
169 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
170 Pharmacology of an original and selective nonpeptide antagonist ligand for the human tachykinin NK2 receptor. Eur J Pharmacol. 2005 Jun 1;516(2):104-11.
171 Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
172 Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochem Pharmacol. 2009 May 1;77(9):1522-30.
173 Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
174 Effects of FK224, a novel compound NK1 and NK2 receptor antagonist, on airway constriction and airway edema induced by neurokinins and sensory nerv... J Pharmacol Exp Ther. 1992 Jul;262(1):403-8.
175 Dual tachykinin NK1/NK2 antagonist DNK333 inhibits neurokinin A-induced bronchoconstriction in asthma patients. Eur Respir J. 2004 Jan;23(1):76-81.
176 Effect of an NK1/NK2 receptor antagonist on airway responses and inflammation to allergen in asthma. Am J Respir Crit Care Med. 2007 Mar 1;175(5):450-7.
177 Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica. 2000 Jun;30(6):627-42.
178 The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43.
179 Mechanisms of modafinil: A review of current research. Neuropsychiatr Dis Treat. 2007 June; 3(3): 349-364.
180 Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002;62(4):633-53.
181 Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol. 1996;49(5):411-5.
182 Induction of prostate apoptosis by alpha1-adrenoceptor antagonists: mechanistic significance of the quinazoline component. Prostate Cancer Prostatic Dis. 2002;5(2):88-95.
183 Bunazosin, a selective alpha1-adrenoceptor antagonist, as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage. Cardiovasc Drug Rev. 2005 Spring;23(1):43-56.
184 The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade. J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):142-50.
185 Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
186 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
187 Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52.
188 Imaging the effects of methylphenidate on brain dopamine: new model on its therapeutic actions for attention-deficit/hyperactivity disorder. Biol Psychiatry. 2005 Jun 1;57(11):1410-5.
189 Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain. Eur J Pharmacol. 2002 Jun 28;447(1):51-7.
190 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31.
191 Rapid detection of Parkinson's disease by SPECT with altropane: a selective ligand for dopamine transporters. Synapse. 1998 Jun;29(2):128-41.
192 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 927).
193 Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5... Endocr Relat Cancer. 2009 Mar;16(1):281-90.
194 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
195 Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
196 5-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58.
197 The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.
198 Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.
199 The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
200 The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011 May 30;2:25.
201 A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015 Apr;13(4):701-8.e1.
202 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
203 Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844.
204 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
205 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
206 Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70.
207 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
208 Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
209 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
210 Effect of serotonin (5-HT)3-receptor antagonists YM060, YM114 (KAE-393), ondansetron and granisetron on 5-HT4 receptors and gastric emptying in rodents. Jpn J Pharmacol. 1995 Nov;69(3):205-14.
211 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
212 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
213 Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
214 JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
215 SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
216 Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
217 A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
218 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
219 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
220 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
221 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
222 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
223 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
224 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3639).
225 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
226 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
227 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
228 Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53.
229 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
230 Role of parasympathetic nerves and muscarinic receptors in allergy and asthma.Chem Immunol Allergy.2012;98:48-69.
231 M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor. Pharmacol Res. 2009 May;59(5):300-5.
232 Muscarinic M3-receptors mediate cholinergic synergism of mitogenesis in airway smooth muscle. Am J Respir Cell Mol Biol. 2003 Feb;28(2):257-62.
233 Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout ... Eur J Pharmacol. 2009 Aug 1;615(1-3):201-6.
234 Interaction of neuromuscular blocking drugs with recombinant human m1-m5 muscarinic receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Nov;125(5):1088-94.
235 Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor ... Am J Physiol Gastrointest Liver Physiol. 2008 Jul;295(1):G112-G123.
236 Mechanism of long-lasting block of ganglion nicotinic receptors by mono-ammonium compounds with long aliphatic chain. J Auton Nerv Syst. 1994 Aug;48(3):231-40.
237 Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6.
238 Epibatidine isomers and analogues: structure-activity relationships. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7.
239 The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13.
240 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization. J Pharmacol Exp Ther. 1994 Jul;270(1):319-28.
241 Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57.
242 Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48.
243 Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. Bioorg Med Chem. 2007 May 15;15(10):3368-72.
244 Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
245 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
246 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
247 Novel anti-obesity drugs. Expert Opin Investig Drugs. 2000 Jun;9(6):1317-26.
248 Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.
249 Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss. J Med Chem. 2023 Mar 9;66(5):3195-3211.
250 The protective effects of the melanocortin receptor (MCR) agonist, melanotan-II (MTII), against binge-like ethanol drinking are facilitated by deletion of the MC3 receptor in mice. Neuropeptides. 2014 Feb;48(1):47-51.
251 Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol. 2009 Feb;156(3):397-411.
252 Novel 1',1'-chain substituted hexahydrocannabinols: 9-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid r... J Med Chem. 2010 Oct 14;53(19):6996-7010.
253 Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism. J Med Chem. 2008 Nov 13;51(21):6970-9.
254 Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
255 Clinical pipeline report, company report or official report of AstraZeneca (2009).
256 Company report (Gwpharm)
257 Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits 9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans.Br J Clin Pharmacol.2013 Jul;76(1):65-77.
258 Clinical pipeline report, company report or official report of Bird Rock Bio.
259 Clinical pipeline report, company report or official report of Affimed Therapeutics.
260 Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
261 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
262 Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76.
263 Coronary circulation responses to binodenoson, a selective adenosine A2A receptor agonist. Am J Cardiol. 2007 Jun 1;99(11):1507-12.
264 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3290).
265 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
266 Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
267 Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.
268 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
269 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
270 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
271 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
272 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
273 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
274 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
275 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
276 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
277 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
278 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
279 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
280 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
281 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
282 Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci. 2015 Jan 15;8:453.
283 AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620.
284 Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12.
285 Acyltransferase inhibitors: a patent review (2010-present).Expert Opin Ther Pat. 2015 Feb;25(2):145-58.
286 [(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors. Br J Pharmacol. 2000 May;130(2):409-17.
287 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
288 Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12.
289 Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects. Am J Physiol Lung Cell Mol Physiol. 2009 Aug;297(2):L340-6.
290 Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
291 Additive protective effects of donepezil and nicotine against salsolinol-induced cytotoxicity in SH-SY5Y cells. Neurotox Res. 2009 Oct;16(3):194-204.
292 Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8.
293 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7354).
294 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
295 Comparison of pharmacological effects of L- and DL-n-butyl-scopolamine in rat uterus. Yao Xue Xue Bao. 1994;29(1):24-7.
296 Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51.
297 Nicotine, brain nicotinic receptors, and neuropsychiatric disorders. Arch Med Res. 2000 Mar-Apr;31(2):131-44.
298 The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
299 Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
300 Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
301 Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
302 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
303 Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
304 SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.
305 5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. J Nat Prod. 2009 Dec;72(12):2172-6.
306 In vivo characterization of the novel neuropeptide Y Y1 receptor antagonist H 409/22. J Cardiovasc Pharmacol. 2000 Oct;36(4):516-25.
307 SR 120819A, an orally-active and selective neuropeptide Y Y1 receptor antagonist. FEBS Lett. 1995 Apr 3;362(2):192-6.
308 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 305).
309 Neuropeptide Y (NPY) Y4 receptor selective agonists based on NPY(32-36): development of an anorectic Y4 receptor selective agonist with picomolar a... J Med Chem. 2006 Apr 20;49(8):2661-5.
310 Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
311 Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
312 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
313 Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.
314 A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
315 Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.
316 Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
317 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
318 Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46.
319 The human MT1 melatonin receptor stimulates cAMP production in the human neuroblastoma cell line SH-SY5Y cells via a calcium-calmodulin signal transduction pathway. J Neuroendocrinol. 2005 Mar;17(3):170-8.
320 MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85.
321 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7393).
322 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 288).
323 Melatonin and sleep in aging population. Exp Gerontol. 2005 Dec;40(12):911-25.
324 Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. Curr Top Med Chem. 2008;8(11):954-68.
325 Luzindole (N-0774): a novel melatonin receptor antagonist. J Pharmacol Exp Ther. 1988 Sep;246(3):902-10.
326 Effects of two melatonin analogues, S-20098 and S-20928, on melatonin receptors in the pars tuberalis of the rat. J Pineal Res. 1998 Oct;25(3):172-6.
327 US patent application no. 5,151,446, Substituted 2-amidotetralins as melatonin agonists and antagonists.
328 Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude. Eur J Pharmacol. 1999 Oct 15;382(3):157-66.