General Information of Drug (ID: DMU34BK)

Drug Name
A-987306 Drug Info
Synonyms
SCHEMBL604437; CHEMBL519240; BDBM26226; MolPort-023-276-880; DJKJVWJQAVGLHJ-YPMHNXCESA-N; ZINC42887577; AKOS024457726; NCGC00370852-01; UNII-6BVK16R925 component DJKJVWJQAVGLHJ-YPMHNXCESA-N; (12S,17S)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetracyclo[8.7.0.0^{2,7}.0^{12,17}]heptadeca-1(10),2(7),3,5-tetraen-4-amine; (-)-(7aS*,11aS*)-4-piperazin-1-yl-5,6,7a,8,9,10,11,11a-octahydro[1]benzofuro[2,3h]quinazolin-2-amine; (+/-)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
44538833
CAS Number
CAS 1082954-71-9
TTD Drug ID
DMU34BK

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)
Drug(s) Targeting Dopamine D3 receptor (D3R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cariprazine DMJYDVK Bipolar disorder 6A60 Approved [2]
Pramipexole DMNMW9R Parkinson disease 8A00.0 Approved [3]
Ropinirole DMA6S1D Parkinson disease 8A00.0 Approved [3]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [4]
P2B-001 DM9PVHX Parkinson disease 8A00.0 Phase 3 [5]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [6]
ONC201 DMM5SCF Endometrial cancer 2C76 Phase 2 [7]
TAK-906 DMBQD9H Diabetic gastroparesis DA41.00 Phase 2 [8]
GSK598809 DMGU05N Drug abuse 6C4G.1Z Phase 2 [9]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [9]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1B receptor (HTR1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [10]
Eletriptan DMW649X Migraine 8A80 Approved [3]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [3]
Frovatriptan DM7RE8P Migraine 8A80 Approved [3]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [3]
Naratriptan DMO50U2 Headache 8A80-8A84 Approved [11]
Prolixin decanoate DMMJ1IS Schizophrenia 6A20 Approved [3]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [12]
NXN-188 DMMBAIH Migraine 8A80 Phase 2 [13]
[N-methyl-3H(3)]AZ-10419369 DMSCV02 Mood disorder 6A60-6E23 Phase 1 [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CCX-354 DMSHV9C Autoimmune diabetes 5A10 Phase 2 [15]
BMS-817399 DMT8L6P Rheumatoid arthritis FA20 Phase 2 [16]
AVE1701 DMJY35M Rheumatoid arthritis FA20 Phase 1 [17]
AZD4818 DM3VFKM Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [18]
MLN3897 DMRA3EZ Rheumatoid arthritis FA20 Discontinued in Phase 2 [17]
COSALANE DMO3486 N. A. N. A. Terminated [19]
BX 471 DM5CGXB Discovery agent N.A. Investigative [20]
Cosalane derivative DMSFXJ8 Discovery agent N.A. Investigative [19]
⏷ Show the Full List of 8 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [21]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [22]
Tropicamide DM1D90W Mydriasis LA11.62 Approved [23]
Diphenidol DMHPWOM Nausea MD90 Approved [24]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [25]
ISOCLOZAPINE DM52CPU Discovery agent N.A. Investigative [26]
FLUMEZAPINE DMW0HOG Discovery agent N.A. Investigative [27]
ISOLOXAPINE DMH1BN4 Discovery agent N.A. Investigative [28]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester DMVEH40 Discovery agent N.A. Investigative [22]
GNF-PF-5618 DMT8VUS Discovery agent N.A. Investigative [29]
⏷ 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 [21]
Fesoterodine fumarate DM13495 Overactive bladder GC50.0 Approved [30]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [31]
Clidinium DMUMQZ0 Abdominal stomach pain DD91.4 Approved [32]
Trihexyphenidyl DMB19L8 Dystonia 8A02 Approved [33]
Oxyphenonium DMMQHOZ Visceral spasms MD81.4 Approved [34]
Benztropine DMGZOVN Parkinson disease 8A00.0 Approved [35]
Glycopyrrolate DM2M3ZA Anaesthesia 9A78.6 Approved [36]
Pirenzepine DMP6M1N Peptic ulcer DA61 Approved [37]
Cycrimine DM8C43Q Parkinson disease 8A00.0 Approved [38]
⏷ 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 [39]
Triflupromazine DMKFQJP Nausea MD90 Approved [40]
Minaprine DM0EP7M Depression 6A70-6A7Z Approved [41]
SPN-812 DMTV7XH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [42]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [43]
PRX-08066 DMR7H2V Pulmonary arterial hypertension BB01.0 Phase 2 [44]
Pyrimidine derivative 29 DMVOYJ8 N. A. N. A. Patented [45]
Pyrimidine derivative 26 DM90WKN N. A. N. A. Patented [45]
Pyrimidine derivative 23 DM5MLQU N. A. N. A. Patented [45]
Pyrimidine derivative 25 DM51MFS N. A. N. A. Patented [45]
⏷ 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 [39]
ZOTEPINE DMF3VXA Anxiety disorder 6B00-6B0Z Approved [46]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [47]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [2]
Lurasidone hydrochloride DMCVPXO Schizophrenia 6A20 Approved [48]
Aniracetam DMOIFW0 Cerebrovascular ischaemia 8B1Z Approved [49]
lumateperone tosylate DMQ8HOJ Schizophrenia 6A20 Approved [50]
Sarpogrelate DMGLP6S Diabetic complication 5A2Y Approved [51]
Pimavanserin DMR7IVC Parkinson disease 8A00.0 Approved [52]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [53]
⏷ 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 [21]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [22]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [31]
Methylscopolamine DM5VWOB Peptic ulcer DA61 Approved [54]
Gallamine Triethiodide DMPO0MS Stabilize muscle contraction FB3Z Approved [55]
FP-1097 DMC1F2T Urinary incontinence MF50.2 Phase 2 [56]
PSD-506 DMT0KB1 Overactive bladder GC50.0 Discontinued in Phase 2 [57]
Otenzepad DMRXHAC Heart failure BD10-BD13 Discontinued in Phase 2 [58]
SCH-211803 DM92E0W Parkinson disease 8A00.0 Discontinued in Phase 1 [59]
Alvameline DMLN0Y5 Alzheimer disease 8A20 Terminated [60]
⏷ 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 [61]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [62]
Rambazole DMP2DNS Psoriasis vulgaris EA90 Phase 2 [63]
Nepadutant DMPMF6L Infantile colics DD93.1 Phase 1/2 [64]
Saredutant DMSRJY3 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [65]
CS-003 DM1AEVT Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [66]
FK-224 DM1JUS0 Asthma CA23 Discontinued in Phase 2 [67]
DNK-333 DM4ZO01 Irritable bowel syndrome DD91.0 Discontinued in Phase 2 [68]
AVE-5883 DM3P84V Asthma CA23 Discontinued in Phase 1/2 [69]
UK-224671 DMDTRJB Urinary incontinence MF50.2 Discontinued in Phase 1 [70]
⏷ 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 [71]
Alosetron DML2A03 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [72]
Tropisetron DMNSJ7V Fibromyalgia MG30.01 Approved [73]
Palonosetron DMBHMOX Nausea MD90 Approved [74]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [73]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [75]
Cilansetron DMP0NGX Irritable bowel syndrome DD91.0 Phase 3 [76]
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [77]
Norcisapride DMJSKUI Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [78]
YM-114 DML2IXO Nausea MD90 Discontinued in Phase 2 [79]
⏷ 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 [80]
ACECLIDINE DMOLNCZ Glaucoma/ocular hypertension 9C61 Approved [21]
Tiotropium DMFDC0Q Chronic obstructive pulmonary disease CA22 Approved [81]
Ipratropium DMFQ320 Obstructive lung disease CA22.Z Approved [82]
Darifenacin DMWXLYZ Overactive bladder GC50.0 Approved [83]
Methacholine Chloride DMGS4QH Asthma CA23 Approved [84]
SMT-D002 DM1I93C Seborrhea ED91.2 Approved [31]
Solifenacin DMG592Q Overactive bladder GC50.0 Approved [85]
Methylscopolamine DM5VWOB Peptic ulcer DA61 Approved [86]
Cevimeline DMWSMND Sjogren syndrome 4A43.20 Approved [87]
⏷ 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 [3]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [88]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [89]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [90]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [2]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [91]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [92]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [93]
Treximet DMU54QB Migraine 8A80 Approved [9]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [4]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Desmopressin DMS3GVE Diabetic complication 5A2Y Approved [94]
Mozavaptan DMZ905C Hyponatraemia 5C72 Approved [95]
Oxytocin DMDL27I Autism spectrum disorder 6A02 Approved [96]
Conivaptan DM1V329 Euvolemic hyponatremia 5C72 Approved [97]
Felypressin DMHLP9C Localisation N.A. Approved [98]
Terlipressin DMT9FH3 Hypertension BA00-BA04 Approved [99]
ATOSIBAN DMB7WYM N. A. N. A. Phase 4 [100]
Balovaptan DMKMTDG Autism spectrum disorder 6A02 Phase 3 [101]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [62]
SSR149415 DMCMD93 Anxiety disorder 6B00-6B0Z Phase 2 [102]
⏷ 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 [103]
Rolofylline DMSZPR3 Heart failure BD10-BD13 Phase 3 [104]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [105]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [106]
SELODENOSON DMQM3IX Cardiac arrhythmias BC9Z Phase 2 [107]
Apaxifylline DMQMV9F Cognitive impairment 6D71 Phase 2 [108]
SLV320 DM867BJ Heart failure BD10-BD13 Phase 2 [109]
DTI-0009 DMV84OK Atrial fibrillation BC81.3 Phase 2 [107]
Capadenoson DMYWO62 Atrial fibrillation BC81.3 Phase 2 [110]
BAY 1067197 DM4JGNH Heart failure BD10-BD13 Phase 2 [111]
⏷ 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 [1]
5-HT 1B receptor (HTR1B) TTK8CXU 5HT1B_HUMAN Inhibitor [1]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Inhibitor [1]
5-HT 2B receptor (HTR2B) TT0K1SC 5HT2B_HUMAN Inhibitor [1]
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Inhibitor [1]
Adenosine A1 receptor (ADORA1) TTK25J1 AA1R_HUMAN Inhibitor [1]
C-C chemokine receptor type 1 (CCR1) TTC24WT CCR1_HUMAN Inhibitor [1]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Inhibitor [1]
Muscarinic acetylcholine receptor M1 (CHRM1) TTZ9SOR ACM1_HUMAN Inhibitor [1]
Muscarinic acetylcholine receptor M2 (CHRM2) TTYEG6Q ACM2_HUMAN Inhibitor [1]
Muscarinic acetylcholine receptor M3 (CHRM3) TTQ13Z5 ACM3_HUMAN Inhibitor [1]
Muscarinic acetylcholine receptor M4 (CHRM4) TTQ3JTF ACM4_HUMAN Inhibitor [1]
Substance-K receptor (TACR2) TTYO0A3 NK2R_HUMAN Inhibitor [1]
Vasopressin V1a receptor (V1AR) TT4TFGN V1AR_HUMAN Inhibitor [1]

References

1 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.
2 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
5 Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 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.
9 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
10 Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
11 Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
12 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
13 Company report (NeurAxon)
14 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
15 Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial. Ann Rheum Dis. 2013 Mar;72(3):337-44.
16 Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis. J Med Chem. 2014 Sep 25;57(18):7550-64.
17 Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
18 Clinical pipeline report, company report or official report of AstraZeneca (2009).
19 Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds. Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62.
20 Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8.
21 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.
22 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. J Med Chem. 1998 Jun 4;41(12):2047-55.
23 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.
24 Diphenidol-related diamines as novel muscarinic M4 receptor antagonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2972-6.
25 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.
26 Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. J Med Chem. 1990 Feb;33(2):809-14.
27 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.
28 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.
29 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.
30 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
31 Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
32 Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
33 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.
34 Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
35 Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60.
36 Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701.
37 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.
38 Capillary gas chromatography of trihexyphenidyl, procyclidine and cycrimine in biological fluids. J Chromatogr. 1989 Sep 29;494:135-42.
39 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.
40 Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
41 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
42 New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
43 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.
44 Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
45 Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
46 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
47 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
48 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
49 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.
50 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
51 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.
52 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.
53 Clinical pipeline report, company report or official report of Lundbeck.
54 Methylacridinium and its cholinergic properties. Neurotox Res. 2009 Nov;16(4):372-7.
55 Cholinergic regulation of the corpora allata in adult male loreyi leafworm Mythimna loreyi. Arch Insect Biochem Physiol. 2002 Apr;49(4):215-24.
56 Clinical pipeline report, company report or official report of FemmePharma.
57 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
58 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.
59 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.
60 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.
61 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.
62 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.
63 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.
64 Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
65 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.
66 Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
67 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.
68 Dual tachykinin NK1/NK2 antagonist DNK333 inhibits neurokinin A-induced bronchoconstriction in asthma patients. Eur Respir J. 2004 Jan;23(1):76-81.
69 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.
70 Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica. 2000 Jun;30(6):627-42.
71 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.
72 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.
73 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
74 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
75 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.
76 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
77 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.
78 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.
79 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.
80 Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53.
81 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
82 Role of parasympathetic nerves and muscarinic receptors in allergy and asthma.Chem Immunol Allergy.2012;98:48-69.
83 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.
84 Muscarinic M3-receptors mediate cholinergic synergism of mitogenesis in airway smooth muscle. Am J Respir Cell Mol Biol. 2003 Feb;28(2):257-62.
85 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.
86 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.
87 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.
88 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
89 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.
90 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
91 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
92 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).
93 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
94 Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88.
95 Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65.
96 Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist. J Biol Chem. 1997 Oct 17;272(42):26536-44.
97 Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23.
98 Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512.
99 Investigational vasopressin receptor modulators in the pipeline. Expert Opin Investig Drugs. 2009 Aug;18(8):1119-31.
100 The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
101 Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder. J Med Chem. 2020 Feb 27;63(4):1511-1525.
102 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
103 Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
104 Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
105 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.
106 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.
107 Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
108 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
109 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.
110 A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
111 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.