General Information of Drug Therapeutic Target (DTT) (ID: TTSQIFT)

DTT Name 5-HT 1A receptor (HTR1A)
Synonyms Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
Gene Name HTR1A
DTT Type
Successful target
[1]
Related Disease
Anxiety disorder [ICD-11: 6B00-6B0Z]
Depression [ICD-11: 6A70-6A7Z]
Hypertension [ICD-11: BA00-BA04]
Migraine [ICD-11: 8A80]
Mood disorder [ICD-11: 6A60-6E23]
BioChemical Class
GPCR rhodopsin
UniProt ID
5HT1A_HUMAN
TTD ID
T78709
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT
RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN
SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RQ
Function
Functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
KEGG Pathway
cAMP signaling pathway (hsa04024 )
Neuroactive ligand-receptor interaction (hsa04080 )
Serotonergic synapse (hsa04726 )
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Serotonin receptors (R-HSA-390666 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
8 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [1]
Flibanserin DM70DTN Mood disorder 6A60-6E23 Approved [2]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [3], [4]
Tertatolol DM2L3D5 Hypertension BA00-BA04 Approved [5]
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [6]
Treximet DMU54QB Migraine 8A80 Approved [7]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [8]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [9]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 Approved Drug(s)
33 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [10]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [11]
SEP-363856 DMG2QP4 Schizophrenia 6A20 Phase 3 [12]
Xaliproden DM1JCW8 Juvenile idiopathic arthritis FA24 Phase 3 [13]
LECOZOTAN HYDROCHLORIDE DMBJ4IZ Cognitive impairment 6D71 Phase 2/3 [14], [15]
Sarizotan DMH7IPW Rett syndrome LD90.4 Phase 2/3 [16]
Ensaculin hydrochloride DMLPRZJ Parkinson disease 8A00.0 Phase 2 [17], [18]
FKB01MD DM2O7NM N. A. N. A. Phase 2 [19]
FKW00GA DMPXH7N Social phobia 6B04 Phase 2 [19]
Mazapertine succinate DMJKHVX Psychotic disorder 6A20-6A25 Phase 2 [16]
MIN-117 DMSLIW6 Major depressive disorder 6A70.3 Phase 2 [20]
MN-305 DMUGN4B Mood disorder 6A60-6E23 Phase 2 [21]
Neu-P11 DMIQDFW Alzheimer disease 8A20 Phase 2 [22]
OPC-14523 DMB1WF3 Bulimia nervosa 6B81 Phase 2 [23]
ORG-13011 DMAWXJT Anxiety disorder 6B00-6B0Z Phase 2 [24], [15]
RP5063 DMKUE8O Schizophrenia 6A20 Phase 2 [25], [26]
S-15535 DMKTLSD Anxiety disorder 6B00-6B0Z Phase 2 [27], [15], [28]
S-16924 DML2D30 Anxiety disorder 6B00-6B0Z Phase 2 [29], [30]
SDZ-MAR-327 DM2YIOE Psychotic disorder 6A20-6A25 Phase 2 [31]
SUN N4057 DMO9LBE Coronary artery disease BA80 Phase 2 [32]
TGBA01AD DMJ2FTU Mood disorder 6A60-6E23 Phase 2 [33]
TGFK08AA DMNXJ5B Generalized anxiety disorder 6B00 Phase 2 [34]
TGFK09SD DMGWE4H Hypoactive sexual desire dysfunction HA00 Phase 2 [35]
TGWOOAA DMI57ZA Generalized anxiety disorder 6B00 Phase 2 [36]
Zalospirone DMJN3BA Anxiety disorder 6B00-6B0Z Phase 2 [37]
1192U90 DM5IPHE Psychotic disorder 6A20-6A25 Phase 1 [38]
AV-965 DMVL87N Alzheimer disease 8A20 Phase 1 [39]
DSP-1053 DMJDP0E Major depressive disorder 6A70.3 Phase 1 [40]
GSK-958108 DM4LR0Y Premature ejaculation HA03.0Z Phase 1 [41]
NLX-101 DMPJMB7 Rett syndrome LD90.4 Phase 1 [42]
SKL-PSY DM8YNI6 Bipolar disorder 6A60 Phase 1 [43]
SSR-181507 DMXQF1T Schizophrenia 6A20 Phase 1 [44]
Umespirone DMTLNGV Anxiety disorder 6B00-6B0Z Phase 1 [45]
------------------------------------------------------------------------------------
⏷ Show the Full List of 33 Clinical Trial Drug(s)
10 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aryl piperazine derivative 1 DM9DJGU N. A. N. A. Patented [46]
Aryl piperazine derivative 14 DMY8NEL N. A. N. A. Patented [46]
Aryl piperazine derivative 15 DMRK4IE N. A. N. A. Patented [46]
Aryl piperazine derivative 16 DM63XHT N. A. N. A. Patented [46]
Aryl piperazine derivative 6 DMZ3DS5 N. A. N. A. Patented [46]
PMID30124346-Compound-13TABLE4 DMHTJVA Attention deficit hyperactivity disorder 6A05.Z Patented [46]
PMID30124346-Compound-34TABLE4 DM2G3VE Attention deficit hyperactivity disorder 6A05.Z Patented [46]
PMID30124346-Compound-60TABLE5 DM3QX0R Dyskinesia MB47.4 Patented [46]
PMID30124346-Compound-LDT66 DMJMTNL Benign prostatic hyperplasia GA90 Patented [46]
PMID30124346-Compound-LDT8 DM5MUNG Benign prostatic hyperplasia GA90 Patented [46]
------------------------------------------------------------------------------------
⏷ Show the Full List of 10 Patented Agent(s)
45 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
LYSERGIC ACID DIETHYLAMIDE DMACMLO Addictive disorder 6C50-6C5Z Withdrawn from market [47]
Bifeprunox DMOQIMS Schizophrenia 6A20 Discontinued in Phase 3 [48]
BMS-181100 DM0HR5W Psychotic disorder 6A20-6A25 Discontinued in Phase 3 [49], [50]
Flesinoxan DMOIP7R Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [51]
Sunepitron DM6M8ZX N. A. N. A. Discontinued in Phase 3 [52]
TIOSPIRONE DME5QDP N. A. N. A. Discontinued in Phase 3 [53]
Adatanserin DMMKFUP Mood disorder 6A60-6E23 Discontinued in Phase 2 [21], [54]
ALNESPIRONE DMT5KBF Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [55], [15]
AP-521 DMWDCG7 Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [56], [15]
DU 125530 DM63UA9 Mood disorder 6A60-6E23 Discontinued in Phase 2 [57]
GSK163090 DMX7DVH Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [7]
LESOPITRON DIHYDROCHLORIDE DMGQJ2U Mood disorder 6A60-6E23 Discontinued in Phase 2 [58]
MAZAPERTINE DMRHYAU N. A. N. A. Discontinued in Phase 2 [59]
PRX-00023 DMN4RV0 Mood disorder 6A60-6E23 Discontinued in Phase 2 [60]
REC-15/3079 DMIEFH0 Urinary incontinence MF50.2 Discontinued in Phase 2 [61]
Robalzotan DMZAISC Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [62]
BINOSPIRONE MESYLATE DM3HRQI Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [63], [15]
DU-29894 DMN9KXU Psychotic disorder 6A20-6A25 Discontinued in Phase 1 [64]
E2101 DMI9NZ3 Cervical dystonia 8A02.0Y Discontinued in Phase 1 [65]
Ebalzotan DMSOH09 Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [66]
Eptapirone DMFGTMR Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [67]
GR-127607 DMRNI6K Migraine 8A80 Discontinued in Phase 1 [68]
Nerisopam DMK5VB2 Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [69]
SLV-313 DMJFWB7 Schizophrenia 6A20 Discontinued in Phase 1 [70]
SUN-8399 DMBCQFH Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [71]
U-93385 DMMSWJ3 Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [72], [15]
A-74283 DMS3R15 Hypertension BA00-BA04 Terminated [74]
A-80426 DMBC3DG N. A. N. A. Terminated [75]
Anpirtoline DM35LJC Pain MG30-MG3Z Terminated [76]
BMY-7378 DMRHCEG N. A. N. A. Terminated [77]
BTS-79018 DMAH3Z9 Schizophrenia 6A20 Terminated [38]
CGS-18102A DM4W3MU Anxiety disorder 6B00-6B0Z Terminated [78]
CP-293019 DMDQBAL N. A. N. A. Terminated [79]
Du-123015 DMX5SN8 Anxiety disorder 6B00-6B0Z Terminated [80]
Gepirone DMGX5Q0 Depression 6A70-6A7Z Terminated [21]
HT-90B DMQINWF Anxiety disorder 6B00-6B0Z Terminated [81]
Ipsapirone DMEJU1L Anxiety disorder 6B00-6B0Z Terminated [82]
LY-293284 DMH21JG Anxiety disorder 6B00-6B0Z Terminated [83]
NAN-190 DMML3J4 N. A. N. A. Terminated [84]
RWJ-25730 DMRQZWN Psychotic disorder 6A20-6A25 Terminated [85]
S-14506 DM05IQU Anxiety disorder 6B00-6B0Z Terminated [86]
SDZ 216-525 DMPUVFH N. A. N. A. Terminated [84]
SLV-307 DMCPDBS Parkinson disease 8A00.0 Terminated [87]
WAY-100635 DMG58FX Eating disorder 6B82 Terminated [88], [57], [89], [90]
WB-4101 DMQU8B1 N. A. N. A. Terminated [91]
------------------------------------------------------------------------------------
⏷ Show the Full List of 45 Discontinued Drug(s)
2 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CM-2236 DMP9EJ7 Post-traumatic stress disorder 6B40 Preclinical [73]
PD-158771 DM682UV Schizophrenia 6A20 Preclinical [38]
------------------------------------------------------------------------------------
176 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(3-Chloro-phenyl)-piperazin-1-yl-methanone DM7U02R Discovery agent N.A. Investigative [92]
(R)-(-)-10-methyl-11-hydroxyaporphine DMYJAM5 Discovery agent N.A. Investigative [93]
(R)-11-Amino-2-methoxyaporphine DMKJWMC Discovery agent N.A. Investigative [94]
(R)-2,11-Diaminoaporphine DM70ZIF Discovery agent N.A. Investigative [94]
(R)-flurocarazolol DM2KBOU Discovery agent N.A. Investigative [95]
(S)-flurocarazolol DM715AS Discovery agent N.A. Investigative [95]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine DMP4DLV Discovery agent N.A. Investigative [96]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane DMDFU6S Discovery agent N.A. Investigative [97]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane DMNLUKS Discovery agent N.A. Investigative [97]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane DM0GRMD Discovery agent N.A. Investigative [97]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane DM5Z6XG Discovery agent N.A. Investigative [97]
1,6-bis(4-phenylpiperazin-1-yl)hexane DMD3EUI Discovery agent N.A. Investigative [97]
1-((S)-2-aminopropyl)-1H-indazol-6-ol DMU83KP Discovery agent N.A. Investigative [98]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine DM31CVR Discovery agent N.A. Investigative [92]
1-(2,5-Dimethoxy-phenyl)-piperazine DMNETHQ Discovery agent N.A. Investigative [92]
1-(2,5-dimethoxyphenyl)propan-2-amine DM043N8 Discovery agent N.A. Investigative [99]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine DMJXKOF Discovery agent N.A. Investigative [100]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine DM9CVX5 Discovery agent N.A. Investigative [101]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine DM6XCPV Discovery agent N.A. Investigative [100]
1-(2-(3-fluorophenoxy)phenyl)piperazine DMXV2KQ Discovery agent N.A. Investigative [100]
1-(2-(4-fluorophenoxy)phenyl)piperazine DMU082P Discovery agent N.A. Investigative [100]
1-(2-(benzyloxy)phenyl)piperazine DM0UZHL Discovery agent N.A. Investigative [100]
1-(2-(phenoxymethyl)phenyl)piperazine DM7Z19T Discovery agent N.A. Investigative [100]
1-(2-Butoxy-phenyl)-piperazine DMT5S2O Discovery agent N.A. Investigative [102]
1-(2-Chloro-phenyl)-piperazine DM5RE71 Discovery agent N.A. Investigative [103]
1-(2-Ethoxy-phenyl)-piperazine DM2P7YX Discovery agent N.A. Investigative [102]
1-(2-Fluoro-phenyl)-piperazine DM94LID Discovery agent N.A. Investigative [102]
1-(2-Isopropoxy-phenyl)-piperazine DM5KAH6 Discovery agent N.A. Investigative [102]
1-(2-Methoxy-phenyl)-4-propyl-piperazine DMCADRI Discovery agent N.A. Investigative [104]
1-(2-Methoxy-phenyl)-piperazine DM3M4RA Discovery agent N.A. Investigative [103]
1-(2-methoxyphenyl)-4-pentylpiperazine DM0EZSR Discovery agent N.A. Investigative [105]
1-(2-phenoxyphenyl)piperazine DMWFCYN Discovery agent N.A. Investigative [100]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine DMX5N3V Discovery agent N.A. Investigative [106]
1-(3-Fluoro-phenyl)-piperazine DM2SNR0 Discovery agent N.A. Investigative [102]
1-(3-Nitro-phenyl)-piperazine DMMJC5E Discovery agent N.A. Investigative [102]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine DMCH6R1 Discovery agent N.A. Investigative [92]
1-(7-Methoxy-naphthalen-2-yl)-piperazine DM1MJCE Discovery agent N.A. Investigative [107]
1-(benzyloxy)-2-(2-phenylethyl)benzene DMVSC3O Discovery agent N.A. Investigative [108]
1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene DMVB7P3 Discovery agent N.A. Investigative [108]
1-Benzyl-4-chroman-2-ylmethyl-piperazine DMAQSBV Discovery agent N.A. Investigative [109]
1-Butyl-4-(2-methoxy-phenyl)-piperazine DM6QULO Discovery agent N.A. Investigative [104]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine DMGKP9Y Discovery agent N.A. Investigative [104]
1-Methyl-1,3-dihydro-indol-2-one DMMX7V8 Discovery agent N.A. Investigative [110]
1-Naphthalen-2-yl-piperazine DMJK0MF Discovery agent N.A. Investigative [96]
1-naphthylpiperazine DM6BIWK Discovery agent N.A. Investigative [107], [96]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine DMOCAUL Discovery agent N.A. Investigative [111]
1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene DM3UHDW Discovery agent N.A. Investigative [108]
2-(2'-methyl-biphenyl-3-yl)-ethylamine DM7HN4Z Discovery agent N.A. Investigative [112]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol DMZNRFG Discovery agent N.A. Investigative [99]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine DM1ULEX Discovery agent N.A. Investigative [101]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine DM1SN37 Discovery agent N.A. Investigative [101]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine DMDI98B Discovery agent N.A. Investigative [99]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine DMYVDJQ Discovery agent N.A. Investigative [101]
2-(3-Bromophenylthio)-N,N-dimethylethanamine DMFETRH Discovery agent N.A. Investigative [113]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine DM4C9H2 Discovery agent N.A. Investigative [99]
2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one DMID9YA Discovery agent N.A. Investigative [109]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine DM79JVK Discovery agent N.A. Investigative [99]
2-(4-Bromo-phenyl)-1-methyl-ethylamine DMB49UP Discovery agent N.A. Investigative [99]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine DMDHFU9 Discovery agent N.A. Investigative [114]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine DM1O0JD Discovery agent N.A. Investigative [115]
2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine DMU0GDY Discovery agent N.A. Investigative [113]
2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol DMF50YH Discovery agent N.A. Investigative [5]
2-phenoxy-3-(piperidin-4-yl)pyridine DM6JNT5 Discovery agent N.A. Investigative [101]
2-Piperazin-1-yl-benzonitrile DM742IJ Discovery agent N.A. Investigative [102]
2-Piperazin-1-yl-phenol DMQT9OK Discovery agent N.A. Investigative [92]
2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine DM1PSRQ Discovery agent N.A. Investigative [108]
3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole DMTDB62 Discovery agent N.A. Investigative [116]
3-(1-Propyl-pyrrolidin-3-yl)-phenol DM4QRV9 Discovery agent N.A. Investigative [111]
3-(2-Amino-propyl)-1H-indol-5-ol DMQPNUM Discovery agent N.A. Investigative [115]
3-(2-Benzylamino-ethoxy)-phenol DMZCTGF Discovery agent N.A. Investigative [117]
3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine DMRDS1U Discovery agent N.A. Investigative [111]
3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one DMFVCOP Discovery agent N.A. Investigative [109]
3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one DM7LMD6 Discovery agent N.A. Investigative [109]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine DM2ETXB Discovery agent N.A. Investigative [101]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one DMKGIQ1 Discovery agent N.A. Investigative [92]
3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol DMDOPVM Discovery agent N.A. Investigative [118]
3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol DMN8C93 Discovery agent N.A. Investigative [118]
3-Naphthalen-1-yl-1-propyl-pyrrolidine DMNZI9R Discovery agent N.A. Investigative [111]
3-Naphthalen-1-yl-pyrrolidine DMCW7F5 Discovery agent N.A. Investigative [111]
3-Phenyl-1-propyl-pyrrolidine DMJ0SVB Discovery agent N.A. Investigative [111]
3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine DMLZ5F1 Discovery agent N.A. Investigative [108]
4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol DMQVOSU Discovery agent N.A. Investigative [119]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine DM9UA0N Discovery agent N.A. Investigative [100]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine DMCR3VM Discovery agent N.A. Investigative [100]
4-(2-(3-chlorophenoxy)phenyl)piperidine DM0IT5E Discovery agent N.A. Investigative [100]
4-(2-(3-fluorophenoxy)phenyl)piperidine DMZMEOG Discovery agent N.A. Investigative [100]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine DM29QLG Discovery agent N.A. Investigative [100]
4-(2-(4-fluorophenoxy)phenyl)piperidine DMFQT9O Discovery agent N.A. Investigative [100]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine DMM2NHZ Discovery agent N.A. Investigative [100]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine DMF3S50 Discovery agent N.A. Investigative [100]
4-(2-(benzyloxy)phenyl)piperidine DMOC7PY Discovery agent N.A. Investigative [100]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine DMQUAP2 Discovery agent N.A. Investigative [101]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine DMUBHRF Discovery agent N.A. Investigative [100]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine DMJ2GW0 Discovery agent N.A. Investigative [100]
4-(2-fluoro-6-phenoxyphenyl)piperidine DMXIGWC Discovery agent N.A. Investigative [100]
4-(2-phenoxyphenyl)piperidine DMB5IFA Discovery agent N.A. Investigative [100]
4-(3-fluoro-2-phenoxyphenyl)piperidine DM1C3NZ Discovery agent N.A. Investigative [100]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [120]
4-Benzyl-1-chroman-2-ylmethyl-piperidine DM6XLZ0 Discovery agent N.A. Investigative [109]
4-Benzyl-1-chroman-3-ylmethyl-piperidine DMAZMPF Discovery agent N.A. Investigative [109]
5,6-dichloro-3,4-dihydroquinazolin-2-amine DMN1S35 Discovery agent N.A. Investigative [121]
5-chloro-3,4-dihydroquinazolin-2-amine DMKEFJ0 Discovery agent N.A. Investigative [121]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine DMGDTNI Discovery agent N.A. Investigative [121]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine DM7FZU2 Discovery agent N.A. Investigative [121]
5-CT DM260KD Discovery agent N.A. Investigative [122]
7-methoxy-1-naphthylpiperazine DM3MXI5 Discovery agent N.A. Investigative [107]
8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine DMFOM10 Discovery agent N.A. Investigative [5]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline DMQIFZC Discovery agent N.A. Investigative [96]
8-Methoxy-2-piperazin-1-yl-quinoline DMNWC29 Discovery agent N.A. Investigative [96]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine DMK6U2V Discovery agent N.A. Investigative [121]
8-Methoxy-quinolin-2-ylamine DMHZ5SB Discovery agent N.A. Investigative [96]
9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine DM1YK42 Discovery agent N.A. Investigative [5]
9-OH-risperidone DMGORXQ Discovery agent N.A. Investigative [123]
A-987306 DMU34BK Discovery agent N.A. Investigative [124]
AGROCLAVINE DMT9FJZ Discovery agent N.A. Investigative [125]
BRL-15572 DMM61Y2 Discovery agent N.A. Investigative [126]
Brolamfetamine DMC4PF0 Discovery agent N.A. Investigative [99]
CGS-19480A DMC41UH Anxiety disorder 6B00-6B0Z Investigative [127], [15]
Chlorophenylpiperazine DMOA8L2 Discovery agent N.A. Investigative [102]
CP 93129 DMSNVKP Discovery agent N.A. Investigative [122]
Cyamemazine DMZ6YPV Discovery agent N.A. Investigative [128]
EDMT DMS3AXK Discovery agent N.A. Investigative [129]
EMD 56551 DM4SEMA Discovery agent N.A. Investigative [130]
ESCHOLTZINE DMPTDHC Discovery agent N.A. Investigative [131]
Etisulergine DMKH8TC Discovery agent N.A. Investigative [132]
FG-5893 DM1NL3Z Discovery agent N.A. Investigative [133]
GR 125,743 DMMX7KL Discovery agent N.A. Investigative [122]
JNJ-10392980 DMZH0K8 Discovery agent N.A. Investigative [134]
L-772,405 DM5O0CM Discovery agent N.A. Investigative [135]
LP-12 DM8ZR17 Discovery agent N.A. Investigative [136]
LP-211 DMKDGLA Discovery agent N.A. Investigative [137]
LP-44 DM0C3SF Discovery agent N.A. Investigative [136]
LY 165,163 DM9IU21 Discovery agent N.A. Investigative [133]
LY433221 DMHQ0T2 Depression 6A70-6A7Z Investigative [138]
MCL-516 DMQA7ZI Discovery agent N.A. Investigative [94]
MPDT DMYX31S Discovery agent N.A. Investigative [129]
N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine DM0JE7H Discovery agent N.A. Investigative [119]
N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine DM2URTK Discovery agent N.A. Investigative [119]
N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide DMCJWQT Discovery agent N.A. Investigative [137]
N-methyllaurotetanine DMWPBKU Discovery agent N.A. Investigative [131]
N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide DMA4L5P Discovery agent N.A. Investigative [139]
nafadotride DM79KLR Discovery agent N.A. Investigative [133]
NPT-500 DMMUY73 Major depressive disorder 6A70.3 Investigative [43]
P-MPPI DMHSWT6 Discovery agent N.A. Investigative [140], [84]
p-[18F]MPPF DM9SNFX Discovery agent N.A. Investigative [141]
PB-28 DMSXZ19 Discovery agent N.A. Investigative [142]
PG-01037 DM2TP4Q Discovery agent N.A. Investigative [143]
PHENYLPIPERAZINE DMWAK1R Discovery agent N.A. Investigative [96]
piribedil DMNP6QD Discovery agent N.A. Investigative [144]
Quipazine DMPY6IG Discovery agent N.A. Investigative [145]
Repinotan DM47TSV Discovery agent N.A. Investigative [146]
RS-30199 DMDC1B4 Discovery agent N.A. Investigative [147]
S-14671 DMHVEJF Discovery agent N.A. Investigative [28]
SB 216641 DMB3R4Z Discovery agent N.A. Investigative [126]
SB 272183 DMOLNQX Discovery agent N.A. Investigative [148]
SB 649915 DM21Z6H Discovery agent N.A. Investigative [149]
SB 714786 DMGHRY0 Discovery agent N.A. Investigative [149]
SB-271046 DM5VJAF Discovery agent N.A. Investigative [150]
SB-656104 DMVOIL5 Discovery agent N.A. Investigative [151]
SEL-73 DMFKE6C Psychiatric disorder 6E8Z Investigative [43]
Serotonin DMOFCRY Discovery agent N.A. Investigative [145]
SNAP-8719 DMCHPMA Discovery agent N.A. Investigative [152]
spiroxatrine DMPHRXQ Discovery agent N.A. Investigative [133]
SR-59026 DMCRVM2 Discovery agent N.A. Investigative [153]
TFMPP DMAC8TP Discovery agent N.A. Investigative [92]
U92016A DM7CJNE Discovery agent N.A. Investigative [154]
UH-232 DM5K6ZE Discovery agent N.A. Investigative [155]
UH-301 DM5NYWV N. A. N. A. Investigative [156]
WAY 100135 DMC6KYF Discovery agent N.A. Investigative [84]
WAY-466 DMMOH51 Discovery agent N.A. Investigative [157]
[11C]WAY100635 DMXIEA1 Discovery agent N.A. Investigative [158]
[3H]8-OH-DPAT DM4KCYU Discovery agent N.A. Investigative [159]
[3H]NLX-112 DMG1TIV Discovery agent N.A. Investigative [160]
[3H]p-MPPF DM2LA9X Discovery agent N.A. Investigative [161]
[3H]robalzotan DMK1TRG Discovery agent N.A. Investigative [162]
[3H]spiperone DMWHEV8 Discovery agent N.A. Investigative [91]
------------------------------------------------------------------------------------
⏷ Show the Full List of 176 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Major depressive disorder 6A20 Pre-frontal cortex 7.48E-01 -1.45E-04 -5.19E-04
Lateral sclerosis 8A00.0 Cervical spinal cord 2.18E-01 -0.11 -0.51
Alzheimer's disease 8A00.0 Entorhinal cortex 1.49E-05 -0.22 -0.58
Schizophrenia 6A20 Pre-frontal cortex 7.49E-01 -0.02 -0.06
Schizophrenia 6A20 Superior temporal cortex 3.45E-01 -0.02 -0.14
Coronary artery disease BA80-BA8Z Peripheral blood 4.62E-01 -0.14 -0.76
Parkinson's disease 8A00.0 Substantia nigra tissue 5.70E-01 -0.13 -0.53
------------------------------------------------------------------------------------
⏷ Show the Full List of DTT Expression Under 7 Diseases

References

1 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
2 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
3 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.
4 Brexpiprazole: First Global Approval.Drugs.2015 Sep;75(14):1687-97.
5 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).
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
8 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
9 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
10 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
11 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
14 A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in... Clin Pharmacol Ther. 2008 Jan;83(1):86-96.
15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
16 Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57.
17 Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58.
18 The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. Pharmacol Biochem Behav. 1998 Jul;60(3):703-7.
19 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
20 Company report (Minerva Neurosciences),MIN-101,Schizophrenia, 6 trials completed; Once a day formulation completed , Phase IIa completed; Phase IIb enrollment ongoing and expected to continue over the last 3 quarters of 2015.
21 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
22 Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
23 Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88.
24 Antagonism of the 5-HT1A receptor stimulus in a conditioned taste aversion procedure. Eur Neuropsychopharmacol. 1999 Jun;9(4):345-9.
25 Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271
26 EFFICACY AND SAFETY OF NOVEL DOPAMINE SEROTONIN STABILIZER RP 5063 IN ACUTE SCHIZOPHRENIA AND SCHIZOAFFECTIVE DISORDER. Schizophrenia Research Volume 153, Supplement 1, April 2014, Pages S22.
27 S 15535, a benzodioxopiperazine acting as presynaptic agonist and postsynaptic 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Br J Pharmacol. 1999 Nov;128(6):1207-14.
28 Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol. 1998 Mar;357(3):205-17.
29 S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1998 Sep;286(3):1341-55.
30 S-16924 [(R)-2-[1-[2-(2,3-dihydro-benzo[1,4]dioxin-5-yloxy)-ethyl]- pyrrolidin-3yl]-1-(4-fluorophenyl)-ethanone], a novel, potential antipsychotic with marked serotonin1A agonist properties: III. Anxiolytic actions in comparison with clozapine and haloperidol. J Pharmacol Exp Ther. 1999 Mar;288(3):1002-14.
31 DOI: 10.1038/sj.mp.4002062
32 Experimental study of pharmacological hypothermia: enhanced neuroprotective effect of a novel 5-HT 1 A agonist SUN N4057 by the pharmacological hypothermia. No To Shinkei. 2001 Sep;53(9):853-8.
33 Company report (Fabrekramer)
34 50 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87.
35 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032503)
36 Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
37 The serotonin 5-HT receptor agonist tandospirone improves executive function in common marmosets. Behav Brain Res. 2015 Jul 1;287:120-6.
38 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
39 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412)
40 DSP-1053, a novel serotonin reuptake inhibitor with 5-HT1A partial agonistic activity, displays fast antidepressant effect with minimal undesirable effects in juvenile rats. Pharmacol Res Perspect. 2015 Jun;3(3):e00142.
41 Clinical pipeline report, company report or official report of GlaxoSmithKline.
42 In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat.Psychopharmacology (Berl).2012 May;221(2):261-72.
43 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: 1).
44 SSR181507, a dopamine D receptor and 5-HT() receptor ligand: evidence for mixed anxiolytic- and antidepressant-like activities.Pharmacol Biochem Behav.2011 Jan;97(3):428-35.
45 The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96.
46 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
47 Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes. J Med Chem. 1995 Mar 17;38(6):958-66.
48 Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Addict Biol.2012 Mar;17(2):274-86.
49 BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40.
50 The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat
51 Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission. Eur Neuropsychopharmacol. 1999 Sep;9(5):427-40.
52 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.
53 Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone. J Med Chem. 1991 Nov;34(11):3316-28.
54 Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. J Med Chem. 1999Dec 16;42(25):5077-94.
55 Chronic alnespirone-induced desensitization of somatodendritic 5-HT1A autoreceptors in the rat dorsal raphe nucleus. Eur J Pharmacol. 1999 Jan 22;365(2-3):165-73.
56 The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats. J Pharmacol Sci. 2015 Jan;127(1):109-16.
57 5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide: a[11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans. J Pharmacol Exp Ther. 2002 Jun;301(3):1144-50.
58 Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 Oct;113(2):425-30.
59 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.
60 PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety.Pharmacol Biochem Behav.2009 Nov;94(1):8-15.
61 N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract. JPharmacol Exp Ther. 2001 Dec;299(3):1027-37.
62 Use of PET and the radioligand [carbonyl-(11)C]WAY-100635 in psychotropic drug development. Nucl Med Biol. 2000 Jul;27(5):515-21.
63 Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology (Berl). 2001 Nov;158(3):224-9.
64 A comparison of the neuro-endocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers. Br J Clin Pharmacol. 1995 Jan;39(1):7-14.
65 In vitro interactions between a potential muscle relaxant E2101 and human cytochromes P450. Drug Metab Dispos. 2002 Jul;30(7):805-13.
66 The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist. J Pharmacol Exp Ther. 2001 Dec;299(3):883-93.
67 The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol. 2005 Nov;19(6):609-13.
68 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531)
69 Simultaneous determination of nerisopam, a novel anxiolytic agent showing polymorphic metabolism, and its N-acetyl metabolite from human plasma by a validated high performance liquid chromatographic method. J Chromatogr B Biomed Appl. 1996 Mar 29;678(1):63-72.
70 Synthesis and dual D2 and 5-HT1A receptor binding affinities of 7-piperazinyl and 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones. Med Chem. 2014;10(5):484-96.
71 Effects of SUN 8399, a potent and selective 5-HT1A agonist, on conflict behavior and ambulatory activity in mice: comparison with those of buspirone, tandospirone and diazepam. Jpn J Pharmacol. 1994 Apr;64(4):273-80.
72 Tolerance development to the vagal-mediated bradycardia produced by 5-HT1A receptor agonists. J Pharmacol Exp Ther. 1994 Nov;271(2):776-81.
73 CN patent application no. 104151292, Indole derivative or a pharmaceutically acceptable salt thereof.
74 Cardiovascular activity of A-74283, a 5-hydroxytryptamine 1A agent, in the spontaneously hypertensive rat. Pharmacology. 1998 Jan;56(1):17-29.
75 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
76 Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl Med Biol. 2006 Apr;33(3):325-32.
77 8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as busp... J Med Chem. 1996 Mar 1;39(5):1125-9.
78 Quantitative determination of CGS 18102A, a new anxiolytic, in human plasma using capillary gas chromatography/mass spectrometry. Biomed Chromatogr. 1992 Sep-Oct;6(5):244-7.
79 Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30.
80 Neither in vivo MRI nor behavioural assessment indicate therapeutic efficacy for a novel 5HT1A agonist in rat models of ischaemic stroke. BMC Neuroscience 2009, 10:82.
81 Pharmacological profile of (-)HT-90B, a novel 5-HT1A receptor agonist/5-HT2 receptor antagonist. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Nov;19(7):1201-16.
82 Chronic voluntary ethanol intake hypersensitizes 5-HT(1A) autoreceptors in C57BL/6J mice. J Neurochem. 2008 Dec;107(6):1660-70.
83 Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity. J Pharmacol Exp Ther. 1994 Sep;270(3):1270-81.
84 Influence of 5-HT1A receptor antagonism on plus-maze behaviour in mice. II. WAY 100635, SDZ 216-525 and NAN-190. Pharmacol Biochem Behav. 1997 Oct;58(2):593-603.
85 Piperazinylalkyl heterocycles as potential antipsychotic agents. J Med Chem. 1995 Oct 13;38(21):4198-210.
86 S 14506: novel receptor coupling at 5-HT(1A) receptors. Neuropharmacology. 2001 Mar;40(3):334-44.
87 Development and validation of a capillary electrophoresis method for the enantiomeric purity determination of SLV307, a basic potential antipsychotic compound. Electrophoresis. 2004 Aug;25(16):2854-9.
88 Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci. 1997;60(9):653-65.
89 Cocaine and serotonin: a role for the 5-HT(1A) receptor site in the mediation of cocaine stimulant effects. Behav Brain Res. 2001 Nov 29;126(1-2):127-33.
90 Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats. Eur J Pharmacol. 2000 Nov 10;408(1):19-23.
91 Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. J Med Chem. 1993 Oct 15;36(21):3161-5.
92 Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4.
93 R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30.
94 Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines. Bioorg Med Chem. 2008 Jul 15;16(14):6675-81.
95 The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacology (Berl). 2001 Aug;157(1):111-4.
96 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80.
97 Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem. 2010 Jun 24;53(12):4803-7.
98 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
99 5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9.
100 Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7.
101 Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7.
102 Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. J Med Chem. 1989 May;32(5):1052-6.
103 Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands. J Med Chem. 1991 Jun;34(6):1850-4.
104 Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new ... J Med Chem. 1994 Aug 19;37(17):2754-60.
105 Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6628-32.
106 The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine. Bioorg Med Chem. 2007 Nov 1;15(21):6659-66.
107 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8.
108 Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. J Med Chem. 2006 Nov 2;49(22):6607-13.
109 Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. J Med Chem. 2005 Jan 13;48(1):266-73.
110 Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity. Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31.
111 Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997).
112 Novel aminoethylbiphenyls as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22.
113 SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling. Bioorg Med Chem. 2010 Mar 1;18(5):1958-67.
114 4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997).
115 A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem. 2003 Sep 11;46(19):4188-95.
116 3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic a... J Med Chem. 1990 Aug;33(8):2087-93.
117 New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates. Bioorg Med Chem Lett. 1998 Feb 3;8(3):295-300.
118 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. J Med Chem. 1992 Oct 30;35(22):3984-90.
119 Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4.
120 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.
121 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
122 Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):682-8.
123 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
124 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.
125 Ergolines as selective 5-HT1 agonists. J Med Chem. 1988 Aug;31(8):1512-9.
126 SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
127 WO patent application no. 2012,0025,83, Method for treating schizophrenia and related diseases with a combination therapy.
128 Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
129 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
130 Diagnosis of migraine with aura, depression and anxiety from allelic variations in dopaminergic genes
131 Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in ... J Nat Prod. 2006 Mar;69(3):432-5.
132 Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-... J Med Chem. 1985 Oct;28(10):1540-2.
133 Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56.
134 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
135 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001.
136 Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21.
137 Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor act... J Med Chem. 2008 Sep 25;51(18):5813-22.
138 Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23.
139 Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands. J Med Chem. 1988 Oct;31(10):1968-71.
140 p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.
141 A 18F-MPPF PET normative database of 5-HT1A receptor binding in men and women over aging. J Nucl Med. 2005 Dec;46(12):1980-9.
142 New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. J Med Chem. 1996 Jan 5;39(1):176-82.
143 Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.
144 Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.
145 Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
146 Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. J Pharmacol Exp Ther. 1998 Mar;284(3):1082-94.
147 Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat. Neuropharmacology. 1998 Jun;37(6):769-80.
148 SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol. 2001 Jul;133(6):797-806.
149 Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80.
150 Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.
151 Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor. Bioorg Med Chem Lett. 2005 Feb 1;15(3):747-50.
152 Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione ... J Med Chem. 2005 Apr 21;48(8):3076-9.
153 Effect of SR 59026A, a new 5-HT(1A) receptor agonist, on sexual activity in male rats. Behav Pharmacol. 1995 Apr;6(3):276-282.
154 Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther. 1994 Nov;271(2):875-83.
155 (Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997).
156 N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. J Med Chem. 1997 Apr 11;40(8):1252-7.
157 Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.
158 [11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS. Brain. 2005 Apr;128(Pt 4):896-905.
159 Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10.
160 [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch Pharmacol. 2010 Oct;382(4):321-30.
161 Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15.
162 Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol. 1998 Nov 6;360(2-3):219-25.