Therapeutic Targets Database
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TTD Target ID: TTDC00292

Target Information
NameAlpha-1A adrenergic receptor    
Type of targetClinical trial target    
SynonymsAlpha 1A-adrenoceptor    
Alpha 1A-adrenoreceptor    
Alpha adrenergic receptor 1c    
Alpha-1C adrenergic receptor    
DiseaseBenign prostate hyperplasia
[ICD9: 600   ICD10: N40]
[1]
Hypertrophic vascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[2]
Drug(s)XatralPhase IVBPH, Japan; Pediatric[3]
Dutasteride & tamsulosinPhase IIIProstate Cancer; Benign prostatic hyperplasia[4]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP35348
FunctionThis alpha-adrenergic receptor mediates its action by association with g proteins that activate a phosphatidylinositol- calcium second messenger system, and its effect is mediated by G(q) and G(11) proteins.    
SequenceMVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+)-NIGULDIPINE[5]
(+/-)-nantenine[6]
(-)-SNAP-5089[5]
(-)-SNAP-5399,   SNAP-5399[5]
(2,6-Dichloro-phenyl)-[7]
(2-Bromo-phenyl)-[7]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl[8]
1- (2-Chloro-phenyl)-piperazine[9]
1- (2-Methoxy-phenyl)-piperazine[9]
1- (3-Fluoro-pyridin-2-yl)-4-methyl-piperazine[8]
1-Pyridin-2-yl-piperazine[8]
2- (4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole[10]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline[11]
4- ([12]
4- ([12]
4- (1-Naphthalen-1-yl-ethyl)-1H-imidazole[13]
4- (1-Naphthalen-1-yl-propyl)-1H-imidazole[12]
4- (1-Naphthalen-1-yl-vinyl)-1H-imidazole[12]
4- (2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole[12]
4- (3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline[11]
4- (3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol[14]
4- (4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol[14]
4- (4-Methyl-indan-1-yl)-1H-imidazole[15]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[16]
4- (4-chlorobenzyl)-2-allylphthalazin-1[17]
4- (4-chlorobenzyl)-2-methylphthalazin-1[17]
4- (4-chlorobenzyl)phthalazin-1[17]
4-Benzo[b]thiophen-4-yl-1H-imidazole[18]
4-Morpholin-2-yl-benzene-1,2-diol[14]
4-benzyl-2-methylphthalazin-1 (2H)-one[17]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine[19]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine[19]
A-119637[5]
A-123189[5]
A-131701[5]
A-315456[5]
ABANOQUIL[20]
AGN-192172[21]
AGN-193080[21]
ATC-0175[22]
BMY-7378[23]
BP-897[24]
CORYNANTHEINE[5]
FLUANISONE[25]
ISOCLOZAPINE[26]
Imidazolidin-2-ylidene-o-tolyl-amine[21]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine[21]
L-765314[5]
L-771688[5]
LEVONORDEFRIN[12]
MAZAPERTINE[27]
MEDETOMIDINE[13]
N- (5-Bromo-quinoxalin-6-yl)-guanidine[21]
NAFTOPIDIL[5]
NIGULDIPINE[28]
OCTOCLOTHEPIN[29]
R-226161[30]
RS-100329[5]
RS-17053[5]
RS-513815[5]
RWJ-25730[27]
RWJ-38063[5]
RWJ-68141[5]
RWJ-68157[5]
RWJ-69736[5]
RX-821002[31]
Ro-11-04253[5]
Ro-700004,   RS-100975[5]
SILODOSIN[5]
SK&F-104078,   SK-104078[28]
SK&F-104856,   SK-104856[28]
SK&F-105854,   SK-105854[5]
SK&F-106686,   SK-106686[28]
SK&F-86466,   SK-86466[28]
SNAP-5036[5]
SNAP-5089[28]
SNAP-5150[5]
SNAP-6201[5]
SNAP-7915[5]
SNAP-8719[23]
SNAP-94847[32]
SPIPERONE[5]
Siramesine[33]
TIOSPIRONE[34]
UH-301[35]
UPIDOSIN[5]
WAY-100135[35]
WB-4101[20]
sunepitron[36]
Agonist4-Methoxyamphetamine[37]
AntagonistDutasteride & tamsulosin[4]
REC2615[38]
Xatral[3]
BinderKMD-3213
MultitargetDutasteride & tamsulosin[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 3Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
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Ref 5Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. To Reference
Ref 6Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference
Ref 7J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. To Reference
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Ref 9J 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. To Reference
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Ref 11Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. To Reference
Ref 12J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine. To Reference
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Ref 16J 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. To Reference
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Ref 21Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995) To Reference
Ref 22Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. Epub 2009 Sep 6.Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. To Reference
Ref 23J 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. To Reference
Ref 24J Med Chem. 2003 Aug 28;46(18):3822-39.Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors. To Reference
Ref 25J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. To Reference
Ref 26J Med Chem. 1997 Dec 5;40(25):4146-53.Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. To Reference
Ref 27J 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. To Reference
Ref 28J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. To Reference
Ref 29J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adrenoceptors. To Reference
Ref 30Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. To Reference
Ref 31J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. To Reference
Ref 32J Med Chem. 2007 Aug 9;50(16):3883-90.Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits. To Reference
Ref 33J Med Chem. 1995 May 26;38(11):1998-2008.Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. To Reference
Ref 34J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. To Reference
Ref 35J 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. To Reference
Ref 36J 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. To Reference
Ref 37Daws LC, Irvine RJ, Callaghan PD, Toop NP, White JM, Bochner F: Differential behavioural and neurochemical effects of para-methoxyamphetamine and 3,4-methylenedioxymethamphetamine in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2000 Aug;24(6):955-77. To Reference
Ref 38Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27. To Reference



 

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