Target Information

Target General Infomation
Target ID
T78709
Former ID
TTDS00098
Target Name
5-hydroxytryptamine 1A receptor
Gene Name
HTR1A
Synonyms
5-HT-1A; 5-HT1A; 5-HT1A receptor; 5-hydroxytryptamine receptor 1A; G-21; Serotonin receptor; Serotonin receptor 1A; HTR1A
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Addiction [ICD code not available]
Aggressive non-hodgkin's lymphoma [ICD9: 200, 201, 202, 202.8, 208.9; ICD10: C81, C81-C86, C82-C85, C91-C95]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alzheimer disease; Peripheral sensory neuropathies; Lateral sclerosis [ICD9:331.0, 356.0, 356.8; ICD10: G30, G64, G90.0, G12.2]
Bulimia nervosa; Severe mood disorders [ICD9: 296, 307.51; ICD10: F30-F39, F50.2]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Cervical dystonia; Spasm [ICD9:333.83, 728.85; ICD10: G24.3, R25.2]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Depression [ICD9: 311; ICD10: F30-F39]
Eating disorder [ICD9: 278, 307.5, 401, 428.0; ICD10: E66, F50, I10-I16, I50]
Female sexual dysfunction [ICD9: 302.7; ICD10: F52]
Generalized anxiety disorder [ICD9: 300, 300.02, 311; ICD10: F32, F40-F42, F41.1]
Generalized anxiety disorder; Social phobia [ICD9: 300, 300.02, 300.23; ICD10: F40-F42, F40.1, F41.1, F93.2]
Hypoactive sexual desire disorder [ICD10: F52.0]
Hypertension [ICD9: 401; ICD10: I10-I16]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Major depressive disorder; Episode; Anxiety [ICD9: 296.2, 296.3, 300; ICD10: F32, F32.2, F32.3, F33, F40-F42]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Mood disorder [ICD10: F30-F39]
Migraine [ICD9: 346; ICD10: G43]
Post-traumatic stress disorder [ICD9: 309.81; ICD10: F43.1]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99]
Parkinson's disease [ICD9: 332; ICD10: G20]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Premature ejaculation [ICD9: 302.75; ICD10: F52.4]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Schizoaffective disorder; Schizophrenia [ICD9: 295, 295.70; ICD10: F20, F25]
Schizophrenia [ICD9: 295; ICD10: F20]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also 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.
BioChemical Class
GPCR rhodopsin
Target Validation
T78709
UniProt ID
P08908
Sequence
MDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA
IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC
TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED
RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT
RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN
SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP
FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC
RQ
Drugs and Mode of Action
Drug(s) Buspirone Drug Info Approved Anxiety disorder [1], [2]
Flibanserin Drug Info Approved Mood disorder [3], [4]
OPC-34712 Drug Info Approved Major depressive disorder [5], [6]
TERTATOLOL Drug Info Approved Hypertension [7], [8]
Trazodone Drug Info Approved Depression [9], [10]
Treximet Drug Info Approved Migraine [11]
Urapidil Drug Info Approved Hypertension [8]
Vilazodone Drug Info Approved Major depressive disorder [12], [13]
CM-2395 Drug Info Phase 3 Schizophrenia [14]
Flibanserin Drug Info Phase 3 Female sexual dysfunction [15], [4]
LECOZOTAN HYDROCHLORIDE Drug Info Phase 2/3 Cognitive disorders [16]
Eltoprazine Drug Info Phase 2 Aggressive non-hodgkin's lymphoma [17]
Ensaculin hydrochloride Drug Info Phase 2 Parkinson's disease [18]
Mazapertine succinate Drug Info Phase 2 Psychotic disorders [19]
MIN-117 Drug Info Phase 2 Major depressive disorder [20]
MN-305 Drug Info Phase 2 Severe mood disorders [21]
Neu-P11 Drug Info Phase 2 Insomnia [22]
OPC-14523 Drug Info Phase 2 Bulimia nervosa; Severe mood disorders [15]
ORG-13011 Drug Info Phase 2 Psychotic disorders [23]
RP5063 Drug Info Phase 2 Schizoaffective disorder; Schizophrenia [24]
S-15535 Drug Info Phase 2 Anxiety disorder [25], [26]
S-16924 Drug Info Phase 2 Anxiety disorder [27], [28], [29]
SDZ-MAR-327 Drug Info Phase 2 Psychotic disorders [30], [31]
SUN N4057 Drug Info Phase 2 Coronary artery disease [32]
TGBA01AD Drug Info Phase 2 Severe mood disorders [21]
TGFK08AA-ER Drug Info Phase 2 Generalized anxiety disorder [33]
TGFK09SD-ER Drug Info Phase 2 Hypoactive sexual desire disorder [34]
TGWOOAA Drug Info Phase 2 Generalized anxiety disorder; Social phobia [35]
Zalospirone Drug Info Phase 2 Anxiety disorder [36], [37]
1192U90 Drug Info Phase 1 Psychotic disorders [38]
AV-965 Drug Info Phase 1 Alzheimer disease [39]
DSP-1053 Drug Info Phase 1 Major depressive disorder [40]
GSK-958108 Drug Info Phase 1 Premature ejaculation [41]
OPC-14523 Drug Info Phase 1 Female sexual dysfunction [15]
SSR-181507 Drug Info Phase 1 Schizophrenia [31]
Umespirone Drug Info Phase 1 Anxiety disorder [42]
CM-2236 Drug Info Preclinical Post-traumatic stress disorder [43]
PD-158771 Drug Info Preclinical Schizophrenia [31]
LYSERGIC ACID DIETHYLAMIDE Drug Info Withdrawn from market Addiction [44], [45]
Bifeprunox Drug Info Discontinued in Phase 3 Schizophrenia [31]
BMS-181100 Drug Info Discontinued in Phase 3 Psychotic disorders [46], [47]
Flesinoxan Drug Info Discontinued in Phase 3 Anxiety disorder [48], [49]
Sunepitron Drug Info Discontinued in Phase 3 Discovery agent [50]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [51], [52]
Xaliproden Drug Info Discontinued in Phase 3 Alzheimer disease; Peripheral sensory neuropathies; Lateral sclerosis [53]
Adatanserin Drug Info Discontinued in Phase 2 Severe mood disorders [21]
ALNESPIRONE Drug Info Discontinued in Phase 2 Anxiety disorder [54]
AP-521 Drug Info Discontinued in Phase 2 Anxiety disorder [55]
DU 125530 Drug Info Discontinued in Phase 2 Mood disorder [56]
GSK163090 Drug Info Discontinued in Phase 2 Major depressive disorder; Episode; Anxiety [57]
LESOPITRON DIHYDROCHLORIDE Drug Info Discontinued in Phase 2 Mood disorder [58]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [59]
PRX-00023 Drug Info Discontinued in Phase 2 Severe mood disorders [21]
REC-15/3079 Drug Info Discontinued in Phase 2 Urinary incontinence [60], [61]
Robalzotan Drug Info Discontinued in Phase 2 Anxiety disorder [62], [63]
Sarizotan Drug Info Discontinued in Phase 2 Parkinson's disease [64]
BINOSPIRONE MESYLATE Drug Info Discontinued in Phase 1 Anxiety disorder [65]
DU-29894 Drug Info Discontinued in Phase 1 Psychotic disorders [66]
E2101 Drug Info Discontinued in Phase 1 Cervical dystonia; Spasm [67]
Ebalzotan Drug Info Discontinued in Phase 1 Anxiety disorder [68]
Eptapirone Drug Info Discontinued in Phase 1 Anxiety disorder [69]
GR-127607 Drug Info Discontinued in Phase 1 Migraine [70]
Nerisopam Drug Info Discontinued in Phase 1 Anxiety disorder [71]
SLV-313 Drug Info Discontinued in Phase 1 Schizophrenia [31]
SUN-8399 Drug Info Discontinued in Phase 1 Anxiety disorder [72]
U-93385 Drug Info Discontinued in Phase 1 Anxiety disorder [73]
1192U90 Drug Info Terminated Schizophrenia [31]
A-74283 Drug Info Terminated Hypertension [74]
A-80426 Drug Info Terminated Discovery agent [75]
Anpirtoline Drug Info Terminated Pain [76]
BMY-7378 Drug Info Terminated Discovery agent [77], [78]
BTS-79018 Drug Info Terminated Schizophrenia [31]
CGS-18102A Drug Info Terminated Anxiety disorder [79]
CP-293019 Drug Info Terminated Discovery agent [80], [81]
Du-123015 Drug Info Terminated Anxiety disorder [82]
Gepirone ER Drug Info Terminated Depression [21]
HT-90B Drug Info Terminated Anxiety disorder [83]
Ipsapirone Drug Info Terminated Anxiety disorder [84], [85]
LY-293284 Drug Info Terminated Anxiety disorder [86], [87]
NAN-190 Drug Info Terminated Discovery agent [88], [89]
RWJ-25730 Drug Info Terminated Psychotic disorders [90]
S-14506 Drug Info Terminated Anxiety disorder [91], [92]
SDZ 216-525 Drug Info Terminated Discovery agent [93], [94]
SDZ-MAR-327 Drug Info Terminated Schizophrenia [31]
SLV-307 Drug Info Terminated Parkinson's disease [95]
WAY 100135 Drug Info Terminated Discovery agent [96], [97]
WAY-100635 Drug Info Terminated Eating disorder [98], [99]
WB-4101 Drug Info Terminated Discovery agent [100], [101]
Sunepitron Drug Info Investigative Unspecified [102]
Inhibitor (3-Chloro-phenyl)-piperazin-1-yl-methanone Drug Info [103]
(R)-(-)-10-methyl-11-hydroxyaporphine Drug Info [104]
(R)-11-Amino-2-methoxyaporphine Drug Info [105]
(R)-2,11-Diaminoaporphine Drug Info [105]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info [106]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info [107]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info [107]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info [107]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info [107]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info [107]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [108]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info [103]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info [103]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info [109]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info [110]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine Drug Info [111]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info [110]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info [110]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info [110]
1-(2-(benzyloxy)phenyl)piperazine Drug Info [110]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info [110]
1-(2-Butoxy-phenyl)-piperazine Drug Info [112]
1-(2-Chloro-phenyl)-piperazine Drug Info [113]
1-(2-Ethoxy-phenyl)-piperazine Drug Info [112]
1-(2-Fluoro-phenyl)-piperazine Drug Info [112]
1-(2-Isopropoxy-phenyl)-piperazine Drug Info [112]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info [114]
1-(2-Methoxy-phenyl)-piperazine Drug Info [113]
1-(2-methoxyphenyl)-4-pentylpiperazine Drug Info [115]
1-(2-phenoxyphenyl)piperazine Drug Info [110]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [116]
1-(3-Fluoro-phenyl)-piperazine Drug Info [112]
1-(3-Nitro-phenyl)-piperazine Drug Info [112]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info [103]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info [103]
1-(7-Methoxy-naphthalen-2-yl)-piperazine Drug Info [117]
1-(benzyloxy)-2-(2-phenylethyl)benzene Drug Info [118]
1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene Drug Info [118]
1-Benzyl-4-chroman-2-ylmethyl-piperazine Drug Info [119]
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info [114]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info [114]
1-Methyl-1,3-dihydro-indol-2-one Drug Info [120]
1-Naphthalen-1-yl-piperazine Drug Info [106]
1-Naphthalen-2-yl-piperazine Drug Info [106]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info [121]
1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene Drug Info [118]
2-(2'-methyl-biphenyl-3-yl)-ethylamine Drug Info [122]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info [109]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info [111]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info [111]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [109]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info [111]
2-(3-Bromophenylthio)-N,N-dimethylethanamine Drug Info [123]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [109]
2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one Drug Info [119]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info [109]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info [109]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info [124]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info [125]
2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine Drug Info [123]
2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol Drug Info [126]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info [111]
2-Piperazin-1-yl-benzonitrile Drug Info [112]
2-Piperazin-1-yl-phenol Drug Info [103]
2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info [118]
3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole Drug Info [127]
3-(1-Propyl-pyrrolidin-3-yl)-phenol Drug Info [121]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info [125]
3-(2-Benzylamino-ethoxy)-phenol Drug Info [128]
3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine Drug Info [121]
3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one Drug Info [119]
3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one Drug Info [119]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info [111]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info [103]
3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info [129]
3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info [129]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info [121]
3-Naphthalen-1-yl-pyrrolidine Drug Info [121]
3-Phenyl-1-propyl-pyrrolidine Drug Info [121]
3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info [118]
4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol Drug Info [130]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info [110]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info [110]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info [110]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info [110]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info [110]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info [110]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info [110]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info [110]
4-(2-(benzyloxy)phenyl)piperidine Drug Info [110]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info [111]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info [110]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info [110]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info [110]
4-(2-phenoxyphenyl)piperidine Drug Info [110]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info [110]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [131]
4-Benzyl-1-chroman-2-ylmethyl-piperidine Drug Info [119]
4-Benzyl-1-chroman-3-ylmethyl-piperidine Drug Info [119]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [132]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [132]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [132]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [132]
8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine Drug Info [126]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info [106]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info [106]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [132]
8-Methoxy-quinolin-2-ylamine Drug Info [106]
9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine Drug Info [126]
A-80426 Drug Info [133]
A-987306 Drug Info [134]
AGROCLAVINE Drug Info [135]
BMY-7378 Drug Info [136]
Brolamfetamine Drug Info [109]
CHLOROPHENYLPIPERAZINE Drug Info [112]
CP-293019 Drug Info [137]
ESCHOLTZINE Drug Info [138]
Etisulergine Drug Info [139]
JNJ-10392980 Drug Info [140]
LYSERGIC ACID DIETHYLAMIDE Drug Info [141]
MAZAPERTINE Drug Info [142]
MCL-516 Drug Info [105]
N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine Drug Info [130]
N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine Drug Info [130]
N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide Drug Info [143]
N-methyllaurotetanine Drug Info [138]
N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide Drug Info [144]
PB-28 Drug Info [145]
PG-01037 Drug Info [146]
PHENYLPIPERAZINE Drug Info [106]
QUIPAZINE Drug Info [147]
SB-271046 Drug Info [148]
SB-656104 Drug Info [149]
SEROTONIN Drug Info [147]
SNAP-8719 Drug Info [150]
SPIPERONE Drug Info [151]
Sunepitron Drug Info [102]
TERTATOLOL Drug Info [126]
TIOSPIRONE Drug Info [152]
UH-232 Drug Info [153]
UH-301 Drug Info [154]
WAY-466 Drug Info [155]
WB-4101 Drug Info [151]
Antagonist (R)-flurocarazolol Drug Info [156]
(S)-flurocarazolol Drug Info [156]
(S)-UH-301 Drug Info [157]
(S)-WAY 100135 Drug Info [157]
9-OH-risperidone Drug Info [158]
AV-965 Drug Info [159]
BINOSPIRONE MESYLATE Drug Info [160], [8]
cyamemazine Drug Info [161]
DSP-1053 Drug Info [162]
DU 125530 Drug Info [163]
GR 125,743 Drug Info [164]
GSK-958108 Drug Info [165]
GSK163090 Drug Info [166]
LECOZOTAN HYDROCHLORIDE Drug Info [167], [8]
LY433221 Drug Info [168]
MIN-117 Drug Info [169]
MPDT Drug Info [170]
NAN-190 Drug Info [157]
ORG-13011 Drug Info [171], [8]
P-MPPI Drug Info [157], [172]
p-[18F]MPPF Drug Info [173]
PD-158771 Drug Info [31]
REC-15/3079 Drug Info [174]
repinotan Drug Info [175]
Robalzotan Drug Info [176]
RP5063 Drug Info [177], [178]
S-15535 Drug Info [179], [8]
SB 272183 Drug Info [180]
SB 649915 Drug Info [181]
SB 714786 Drug Info [181]
SDZ 216-525 Drug Info [157]
SLV-307 Drug Info [182]
TGWOOAA Drug Info [183]
Treximet Drug Info [166]
Umespirone Drug Info [184]
WAY 100135 Drug Info [157]
WAY-100635 Drug Info [185], [186], [163]
Xaliproden Drug Info [187]
[11C]WAY100635 Drug Info [188]
[3H]p-MPPF Drug Info [189]
[3H]robalzotan Drug Info [190]
[3H]WAY100635 Drug Info [191]
Agonist 1-naphthylpiperazine Drug Info [117]
1192U90 Drug Info [31]
5-CT Drug Info [164]
7-methoxy-1-naphthylpiperazine Drug Info [117]
A-74283 Drug Info [192]
Adatanserin Drug Info [193], [21]
ALNESPIRONE Drug Info [194], [8]
AP-521 Drug Info [195], [8]
BRL-15572 Drug Info [196]
Buspirone Drug Info [197]
CM-2236 Drug Info [198]
CM-2395 Drug Info [199]
CP 93129 Drug Info [164]
Dual norepinephrine reuptake inhibitors/5-HT1A partial agonists Drug Info [200]
Ebalzotan Drug Info [201]
Eltoprazine Drug Info [202]
EMDT Drug Info [170]
Eptapirone Drug Info [203]
FG-5893 Drug Info [204]
Flesinoxan Drug Info [205]
Gepirone ER Drug Info [21]
GR-127607 Drug Info [206]
Ipsapirone Drug Info [207]
L-772,405 Drug Info [208]
LESOPITRON DIHYDROCHLORIDE Drug Info [209]
LP-12 Drug Info [210]
LP-211 Drug Info [143]
LP-44 Drug Info [210]
LY 165,163 Drug Info [204]
LY-293284 Drug Info [211]
MN-305 Drug Info [21]
nafadotride Drug Info [204]
Nerisopam Drug Info [212]
Neu-P11 Drug Info [213]
piribedil Drug Info [214]
S-14671 Drug Info [215]
SB 216641 Drug Info [196]
spiroxatrine Drug Info [204]
SUN N4057 Drug Info [216]
SUN-8399 Drug Info [217]
U-93385 Drug Info [218], [8]
U92016A Drug Info [219]
Urapidil Drug Info [220]
Zalospirone Drug Info [36]
[3H]8-OH-DPAT Drug Info [221]
[3H]NLX-112 Drug Info [222]
[3H]S-15535 Drug Info [215]
Modulator Anpirtoline Drug Info [76]
Bifeprunox Drug Info
BMS-181100 Drug Info
CGS-18102A Drug Info [223]
CGS-19480A Drug Info [224], [8]
Du-123015 Drug Info [225]
DU-29894 Drug Info [226]
E2101 Drug Info [227]
EMD 56551 Drug Info
Ensaculin hydrochloride Drug Info [18]
Flibanserin Drug Info [3]
HT-90B Drug Info [228]
Mazapertine succinate Drug Info
NLX-101 Drug Info
NPT-500 Drug Info [200]
OPC-14523 Drug Info [229]
OPC-34712 Drug Info
PRX-00023 Drug Info
RWJ-25730 Drug Info
S-14506 Drug Info
S-16924 Drug Info [27], [28]
Sarizotan Drug Info
SDZ-MAR-327 Drug Info
SEL-73 Drug Info [200]
SKL-PSY Drug Info [200]
SLV-313 Drug Info
SR-59026 Drug Info
SSR-181507 Drug Info
TGBA01AD Drug Info
TGFK08AA-ER Drug Info [230]
TGFK09SD-ER Drug Info [231]
Trazodone Drug Info [232]
Vilazodone Drug Info [12]
Binder BTS-79018 Drug Info [31]
Modulator (allosteric modulator) RS-30199 Drug Info [233]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Serotonergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT1 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (i) signalling events
WikiPathways Serotonin HTR1 Group and FOS Pathway
SIDS Susceptibility Pathways
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
REF 1Glutamate and anxiety disorders. Curr Psychiatry Rep. 2007 Aug;9(4):278-83.
REF 2(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: 36).
REF 32013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
REF 4(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: 8182).
REF 5ClinicalTrials.gov (NCT01397786) Safety and Tolerability Study of Oral OPC-34712 as Maintenance Treatment in Adults With Schizophrenia. U.S. National Institutes of Health.
REF 6(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: 7672).
REF 7(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: 64).
REF 8Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 9Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
REF 10(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: 213).
REF 11FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021926.
REF 122011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
REF 13(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: 7427).
REF 14Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010.
REF 15Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27.
REF 16ClinicalTrials.gov (NCT00277810) Study Evaluating the Safety, Tolerability, and Efficacy of Lecozotan SR in Outpatients With Alzheimer's Disease. U.S. National Institutes of Health.
REF 17ClinicalTrials.gov (NCT01266174) Effects of Eltoprazine on Cognitive Impairment Associated With Schizophrenia (CIAS) in Adults. U.S. National Institutes of Health.
REF 18Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58.
REF 19Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. J Med Chem. 1998 Jun 4;41(12):1997-2009.
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037483)
REF 21Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 22ClinicalTrials.gov (NCT01489969) Sleep Laboratory Study to Investigate the Safety and Efficacy of Neu-P11 in Primary Insomnia Patients. U.S. National Institutes of Health.
REF 23ClinicalTrials.gov (NCT00000189) Gepirone vs Placebo in Treatment of Cocaine Dependence - 3. U.S. National Institutes of Health.
REF 24ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.
REF 25(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: 26).
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002186)
REF 27S-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.
REF 28S 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.
REF 29(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: 167).
REF 30Positron emission tomographic analysis of central dopamine D1 receptor binding in normal subjects treated with the atypical neuroleptic, SDZ MAR 327. Int J Mol Med. 1998 Jan;1(1):243-7.
REF 31The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
REF 32ClinicalTrials.gov (NCT00272909) Efficacy of SUN N4057 in Subjects With Acute Ischemic Stroke and Measurable Penumbra on Magnetic Resonance Imaging (MRI). U.S. National Institutes of Health.
REF 33Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
REF 34Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
REF 35Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
REF 36The serotonin 5-HT?? receptor agonist tandospirone improves executive function in common marmosets. Behav Brain Res. 2015 Jul 1;287:120-6.
REF 37(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: 58).
REF 381192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412)
REF 40ClinicalTrials.gov (NCT01774747) A Multiple Ascending Oral Dose Evaluation of the Safety, Tolerability, and Pharmacokinetics of DSP-1053 and Its Metabolites in Healthy Subjects and in Subjects With Major Depressive Disorder. U.S. National Institutes of Health.
REF 41ClinicalTrials.gov (NCT00664365) FTIH Study With GSK958108. U.S. National Institutes of Health.
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000698)
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029346)
REF 44Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10.
REF 45(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: 17).
REF 46(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: 8).
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000679)
REF 48(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: 1).
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001126)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004255)
REF 51(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: 101).
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001601)
REF 54Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001421)
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004776)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014469)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026154)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001441)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
REF 60(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: 74).
REF 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010455)
REF 62(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: 72).
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006370)
REF 64Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000677)
REF 66Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001422)
REF 67Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013610)
REF 68Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006909)
REF 69Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010848)
REF 70Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531)
REF 71Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001415)
REF 72Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001433)
REF 73Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002172)
REF 74Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002258)
REF 75Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017)
REF 76Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl Med Biol. 2006 Apr;33(3):325-32. Epub 2006 Mar 9.
REF 77(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: 9).
REF 78Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001317)
REF 79Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001927)
REF 80(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: 977).
REF 81Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008823)
REF 82Neither 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.
REF 83Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003558)
REF 84(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: 42).
REF 85Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000695)
REF 86(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: 19).
REF 87Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003567)
REF 88(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: 73).
REF 89Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001193)
REF 90Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001430)
REF 91(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: 24).
REF 92Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001368)
REF 93(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: 78).
REF 94Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001469)
REF 95Pharmacokinetics, Pharmacodynamics and Tolerance of SLV 307 After Single Oral Administration in Healthy Male Volunteers. Clinical Pharmacology &#38 Therapeutics. 02/1999; 65(2).
REF 96(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: 79).
REF 97Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002060)
REF 98(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: 80).
REF 99Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002783)
REF 100(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: 499).
REF 101Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004048)
REF 102J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
REF 103J Med Chem. 1986 May;29(5):630-4.Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
REF 104Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30. Epub 2007 May 23.R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.
REF 105Bioorg Med Chem. 2008 Jul 15;16(14):6675-81. Epub 2008 Jun 5.Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines.
REF 106J Med Chem. 1986 Nov;29(11):2375-80.5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
REF 107J Med Chem. 2010 Jun 24;53(12):4803-7.Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
REF 108J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
REF 109J Med Chem. 1986 Feb;29(2):194-9.5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.
REF 110Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. Epub 2009 Oct 12.Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
REF 111Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. Epub 2009 Dec 6.Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
REF 112J Med Chem. 1989 May;32(5):1052-6.Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.
REF 113J Med Chem. 1991 Jun;34(6):1850-4.Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
REF 114J Med Chem. 1994 Aug 19;37(17):2754-60.Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs.
REF 115Bioorg Med Chem Lett. 2010 Nov 15;20(22):6628-32. Epub 2010 Sep 21.Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors.
REF 116Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine.
REF 117J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
REF 118J Med Chem. 2006 Nov 2;49(22):6607-13.Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
REF 119J Med Chem. 2005 Jan 13;48(1):266-73.Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
REF 120Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31.Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity.
REF 121Regioselective 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).
REF 122Bioorg Med Chem Lett. 2007 Jun 1;17(11):3018-22. Epub 2007 Mar 23.Novel aminoethylbiphenyls as 5-HT7 receptor ligands.
REF 123Bioorg Med Chem. 2010 Mar 1;18(5):1958-67. Epub 2010 Jan 18.SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling.
REF 1244-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997).
REF 125J Med Chem. 2003 Sep 11;46(19):4188-95.A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
REF 126Synthesis 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).
REF 127J Med Chem. 1990 Aug;33(8):2087-93.3-(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 analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
REF 128Bioorg Med Chem Lett. 1998 Feb 3;8(3):295-300.New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.
REF 129J Med Chem. 1992 Oct 30;35(22):3984-90.6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists.
REF 130Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. Epub 2007 Aug 22.Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
REF 131J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential.
REF 132Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
REF 133J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 134J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia.
REF 135J Med Chem. 1988 Aug;31(8):1512-9.Ergolines as selective 5-HT1 agonists.
REF 136J Med Chem. 1996 Mar 1;39(5):1125-9.8-[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 buspirone.
REF 137Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30.Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
REF 138J Nat Prod. 2006 Mar;69(3):432-5.Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
REF 139J Med Chem. 1985 Oct;28(10):1540-2.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-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
REF 140J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
REF 141J Med Chem. 1995 Mar 17;38(6):958-66.Stereoselective LSD-like activity in a series of d-lysergic acid amides of (R)- and (S)-2-aminoalkanes.
REF 142J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
REF 143J Med Chem. 2008 Sep 25;51(18):5813-22.Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
REF 144J Med Chem. 1988 Oct;31(10):1968-71.Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands.
REF 145J Med Chem. 1996 Jan 5;39(1):176-82.New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
REF 146J Med Chem. 2007 Aug 23;50(17):4135-46. Epub 2007 Aug 2.Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
REF 147J Med Chem. 2009 Nov 12;52(21):6946-50.Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
REF 148Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
REF 149Bioorg Med Chem Lett. 2005 Feb 1;15(3):747-50.Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
REF 150J Med Chem. 2005 Apr 21;48(8):3076-9.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 as selective alpha(1d)-adrenergic receptor antagonists.
REF 151J Med Chem. 1993 Oct 15;36(21):3161-5.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.
REF 152J Med Chem. 1991 Nov;34(11):3316-28.Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone.
REF 153(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997).
REF 154J Med Chem. 1997 Apr 11;40(8):1252-7.N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
REF 155J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
REF 156The 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.
REF 157Influence 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.
REF 158Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
REF 159Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025412)
REF 160Quantifying the 5-HT1A agonist action of buspirone in man. Psychopharmacology (Berl). 2001 Nov;158(3):224-9.
REF 161Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
REF 162DSP-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.
REF 1635-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.
REF 164Agonist 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.
REF 165Clinical pipeline report, company report or official report of GlaxoSmithKline.
REF 166Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 167A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in healthy young and elderly subjects, and in patientswith Alzheimer's disease. Clin Pharmacol Ther. 2008 Jan;83(1):86-96. Epub 2007 May 16.
REF 168Serotonin 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.
REF 169Company 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.
REF 1702-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 171Antagonism of the 5-HT1A receptor stimulus in a conditioned taste aversion procedure. Eur Neuropsychopharmacol. 1999 Jun;9(4):345-9.
REF 172p-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.
REF 173A 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.
REF 174N-[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.
REF 175Characterization 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.
REF 176Use of PET and the radioligand [carbonyl-(11)C]WAY-100635 in psychotropic drug development. Nucl Med Biol. 2000 Jul;27(5):515-21.
REF 177Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271
REF 178EFFICACY 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.
REF 179S 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.
REF 180SB-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.
REF 181Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem. 2005 May 19;48(10):3478-80.
REF 182Development 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.
REF 183Clinical pipeline report, company report or official report of Fabre-Kramer Pharmaceuticals.
REF 184The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96.
REF 185Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats. Eur J Pharmacol. 2000 Nov 10;408(1):19-23.
REF 186Cocaine 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.
REF 187Pharma & Vaccines. Product Development Pipeline. April 29 2009.
REF 188[11C]-WAY100635 PET demonstrates marked 5-HT1A receptor changes in sporadic ALS. Brain. 2005 Apr;128(Pt 4):896-905. Epub 2005 Feb 2.
REF 189Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15.
REF 190Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol. 1998 Nov 6;360(2-3):219-25.
REF 191Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci. 1997;60(9):653-65.
REF 192Cardiovascular activity of A-74283, a 5-hydroxytryptamine 1A agent, in the spontaneously hypertensive rat. Pharmacology. 1998 Jan;56(1):17-29.
REF 193Synthesis 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.
REF 194Chronic 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.
REF 195The 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.
REF 196SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
REF 197Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
REF 198CN patent application no. 104151292, Indole derivative or a pharmaceutically acceptable salt thereof.
REF 199Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
REF 200(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).
REF 201The 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.
REF 202Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
REF 203The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol. 2005 Nov;19(6):609-13.
REF 204Agonist 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.
REF 205Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission. Eur Neuropsychopharmacol. 1999 Sep;9(5):427-40.
REF 206Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003531)
REF 207Chronic voluntary ethanol intake hypersensitizes 5-HT(1A) autoreceptors in C57BL/6J mice. J Neurochem. 2008 Dec;107(6):1660-70.
REF 2083-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem. 1999 Dec 2;42(24):4981-5001.
REF 209Effect 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.
REF 210Structure-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. Epub 2007 Jul 25.
REF 211Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity. J Pharmacol Exp Ther. 1994 Sep;270(3):1270-81.
REF 212Simultaneous 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.
REF 213Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
REF 214Differential 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.
REF 215Labelling 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.
REF 216Experimental 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.
REF 217Effects 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.
REF 218Tolerance development to the vagal-mediated bradycardia produced by 5-HT1A receptor agonists. J Pharmacol Exp Ther. 1994 Nov;271(2):776-81.
REF 219Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther. 1994 Nov;271(2):875-83.
REF 220Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
REF 221Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10.
REF 222[(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.
REF 223Quantitative 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.
REF 224WO patent application no. 2012,0025,83, Method for treating schizophrenia and related diseases with a combination therapy.
REF 225Neither 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.
REF 226A 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.
REF 227In vitro interactions between a potential muscle relaxant E2101 and human cytochromes P450. Drug Metab Dispos. 2002 Jul;30(7):805-13.
REF 228Pharmacological profile of (-)HT-90B, a novel 5-HT1A receptor agonist/5-HT2 receptor antagonist. Prog Neuropsychopharmacol Biol Psychiatry. 1995 Nov;19(7):1201-16.
REF 229Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88.
REF 23050 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87. doi: 10.1038/nrd4075.
REF 231Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032503)
REF 232Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 233Interaction 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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.