Therapeutic Targets Database
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TTD Target ID: TTDS00098

Target Information
Name5-hydroxytryptamine 1A receptor    
Type of targetSuccessful target    
Synonyms5-HT-1A    
5-HT1A    
5-HT1A receptor    
5-hydroxytryptamine receptor 1A    
G-21    
Serotonin receptor    
Serotonin receptor 1A    
DiseaseAnxiety disorder, unspecified    [1]
Brain ischemia    [2]
Cocaine dependence    [3]
Depression    [4]
Detrusor hyperreflexia    [5]
Mood [affective] disorders    [6]
Skeletal muscle associated spasticity    [7]
Urinary incontinence    [5]
Drug(s)BuspironeApprovedAnxiety disorder[8]
TreximetApprovedMigraine[9]
VilazodonePhase III completedMajor Depressive Disorder[10][11]
XaliprodenPhase III completedAlzheimer Disease,Peripheral sensory neuropathies[12]
FlibanserinPhase IIIFemale sexual dysfunction[13]
GSK163090Phase IIMajor Depressive Disorder & Major Depressive Episode & Anxiety[9]
MN-305Phase IISevere Mood Disorders[10]
OPC-14523Phase IIBulimia nervosa OCD MDD, Severe Mood Disorders[14]
TGBA01ADPhase IISevere Mood Disorders[10]
OPC-14523Phase IFemale sexual dysfunction[14]
SSR-181507Phase ISchizophrenia[15]
1192U90DiscontinuedSchizophrenia[15]
AdatanserinDiscontinued in Phase IISevere Mood Disorders[10][16]
BifeprunoxTeminated in Phase IIISchizophrenia[15][17]
PRX-00023Discontinued in Phase IISevere Mood Disorders[10]
SLV-313Terminated in Phase ISchizophrenia[15]
SLV-319Suspended in Phase IObesity, Psychosis[18]
SarizotanDiscontinued in Phase IIParkinsoní»s Disease[19]
Abaperidone hydrochlorideNo development reportedSchizophrenia[15]
BTS-79018No development reportedSchizophrenia[15]
Gepirone ERFDA non-approvable letterDepression[10]
SDZ-MAR-327No development reportedSchizophrenia[15]
PD-158771PreclinicalSchizophrenia[15]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP08908
FunctionThis is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase.    
SequenceMDVLSPGQGNNTTSPPAPFETGGNTTGISDVTVSYQVITSLLLGTLIFCAVLGNACVVAA IALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCC TSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPED RSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVKKVEKTGADT RHGASPAPQPKKSVNGESGSRNWRLGVESKAGGALCANGAVRQGDDGAALEVIEVHRVGN SKEHLPLPSEAGPTPCAPASFERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLP FFIVALVLPFCESSCHMPTLLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFC RQ
Related US Patent6,346,622
6,448,268
6,656,951
6,664,274
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (R)-11-Amino-2-methoxyaporphine[20]
(R)-2,11-Diaminoaporphine[20]
1- (2-Butoxy-phenyl)-piperazine[21]
1- (2-Chloro-phenyl)-piperazine[22]
1- (2-Ethoxy-phenyl)-piperazine[21]
1- (2-Fluoro-phenyl)-piperazine[21]
1- (2-Methoxy-phenyl)-piperazine[22]
1- (2-phenoxyphenyl)piperazine[23]
1- (3-Fluoro-phenyl)-piperazine[21]
1- (3-Nitro-phenyl)-piperazine[21]
1-Methyl-1,3-dihydro-indol-2-one[24]
1-Naphthalen-1-yl-piperazine[25]
1-Naphthalen-2-yl-piperazine[25]
2-Piperazin-1-yl-benzonitrile[21]
2-Piperazin-1-yl-phenol[26]
2-phenoxy-3- (piperidin-4-yl)pyridine[27]
3- (1-Propyl-pyrrolidin-3-yl)-phenol[28]
3- (2-Amino-propyl)-1H-indol-5-ol[29]
3- (2-Benzylamino-ethoxy)-phenol[30]
3-Naphthalen-1-yl-1-propyl-pyrrolidine[28]
3-Naphthalen-1-yl-pyrrolidine[28]
3-Phenyl-1-propyl-pyrrolidine[28]
4- (2-[23]
4- (2-fluoro-6-phenoxyphenyl)piperidine[23]
4- (2-phenoxyphenyl)piperidine[23]
A-80426[31]
A-987306[32]
AGROCLAVINE[33]
ATC-0175[34]
BMY-7378[35]
BP-897[36]
Brolamfetamine[37]
CGS-12066B[38]
CHLOROPHENYLPIPERAZINE[21]
CP-293019[39]
ESCHOLTZINE[40]
Etisulergine[41]
GR-127935[42]
JNJ-10392980[43]
L-745870[44]
LY-334370[45]
LYSERGIC ACID DIETHYLAMIDE[46]
MAZAPERTINE[47]
MCL-516[20]
N-methyllaurotetanine[40]
PB-28[48]
PG-01037[49]
PHENYLPIPERAZINE[25]
PNU-95666E[50]
QUIPAZINE[51]
RU-24969[38]
RWJ-25730[47]
SB-271046[52]
SB-656104[53]
SEROTONIN[51]
SNAP-8719[54]
SPIPERONE[55]
TERTATOLOL[56]
TIOSPIRONE[57]
UH-232[58]
UH-301[59]
WAY-100135[59]
WAY-466[60]
WB-4101[55]
sunepitron[61]
Agonist1192U90[15]
Adatanserin[10][16]
Bifeprunox[15][17]
Buspirone[8]
Flibanserin[13]
Gepirone[62]
Gepirone ER[10]
Ipsapirone[63]
MN-305[10]
OPC-14523[14]
PRX-00023[10]
SDZ-MAR-327[15]
SLV-313[15]
SUN N4057[2]
Sarizotan[19]
TGBA01AD[10]
Urapidil[64]
Antagonist (S)-UH-301[1]
(S)-WAY 100135[1]
Abaperidone hydrochloride[15]
DU 125530[6]
GSK163090[9]
LY433221[11]
NAN-190[1]
P-MPPI[65][1]
PD-158771[15]
Robalzotan[4]
Robalzotan monohydrobromide[4]
SDZ 216-525[1]
SLV-319[18]
Treximet[9]
Vilazodone[10][11]
WAY 100135[1]
WAY-100635[6][3][66]
Xaliproden[12]
BinderBTS-79018[15]
SSR-181507[15]
Multitarget1192U90[15]
Abaperidone hydrochloride[15]
Adatanserin[10][16]
BTS-79018[15]
Bifeprunox[15][17]
Flibanserin[13]
OPC-14523[14]
PD-158771[15]
PRX-00023[10]
SDZ-MAR-327[15]
SLV-313[15]
SLV-319[18]
SSR-181507[15]
Sarizotan[19]
TGBA01AD[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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