Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00030

Target Information
NameAlpha-1D adrenergic receptor    
Type of targetSuccessful target    
SynonymsAlpha 1D-adrenoceptor    
Alpha 1D-adrenoreceptor    
Alpha adrenergic receptor 1a    
Alpha-1A adrenergic receptor    
DiseaseHypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[1]
Drug(s)AlfuzosinApprovedBenign prostatic hyperplasia[2]
DoxazosinApprovedHypertension[3]
TerazosinApprovedBenign prostatic hyperplasia[4][5]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP25100
FunctionThis alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.    
SequenceMTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE AVSLGVPHEVAEGATCQAYELADYSNLRETDI
Related US Patent6,320,049
6,323,231
6,326,372
6,358,959
6,420,366
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[6]
(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-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline[10]
4- ([11]
4- ([11]
4- (1-Naphthalen-1-yl-ethyl)-1H-imidazole[12]
4- (1-Naphthalen-1-yl-propyl)-1H-imidazole[11]
4- (1-Naphthalen-1-yl-vinyl)-1H-imidazole[11]
4- (2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole[11]
4- (3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline[10]
4- (3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol[13]
4- (4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol[13]
4- (4-Methyl-indan-1-yl)-1H-imidazole[14]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[15]
4- (4-chlorobenzyl)-2-allylphthalazin-1[16]
4- (4-chlorobenzyl)-2-methylphthalazin-1[16]
4- (4-chlorobenzyl)phthalazin-1[16]
4-Benzo[b]thiophen-4-yl-1H-imidazole[17]
4-Morpholin-2-yl-benzene-1,2-diol[13]
4-benzyl-2-methylphthalazin-1 (2H)-one[16]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine[18]
6-hydroxy-3- (3',5'-dihydroxyphenyl)coumarin[19]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine[18]
ABANOQUIL[20]
AGN-192172[21]
AGN-193080[21]
BMY-7378[22]
BP-897[23]
CORYNANTHEINE[24]
FLUANISONE[25]
INDORAMIN[20]
ISOCLOZAPINE[26]
Imidazolidin-2-ylidene-o-tolyl-amine[21]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine[21]
LEVONORDEFRIN[11]
MAZAPERTINE[27]
MEDETOMIDINE[12]
N- (5-Bromo-quinoxalin-6-yl)-guanidine[21]
NIGULDIPINE[24]
OCTOCLOTHEPIN[28]
RWJ-25730[27]
RWJ-38063[29]
RWJ-68157[29]
RWJ-69736[29]
RX-821002[30]
SK&F-104078,   SK-104078[24]
SK&F-104856,   SK-104856[24]
SK&F-105854,   SK-105854[24]
SK&F-106686,   SK-106686[24]
SK&F-86466,   SK-86466[24]
SNAP-5089[24]
SNAP-8719[22]
Siramesine[31]
TIOSPIRONE[32]
UH-301[33]
WAY-100135[33]
WB-4101[20]
sunepitron[34]
Agonist4-Methoxyamphetamine[35]
AntagonistAlfuzosin[2]
Doxazosin[3]
Terazosin[4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Differential response to chloroethylclonidine in blood vessels of normotensive and spontaneously hypertensive rats: role of alpha 1D- and alpha 1A-adrenoceptors in contraction. Br J Pharmacol. 2000 Feb;129(4):653-60. To Reference
Ref 2Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002;62(4):633-53. To Reference
Ref 3The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43. To Reference
Ref 4Induction of prostate apoptosis by alpha1-adrenoceptor antagonists: mechanistic significance of the quinazoline component. Prostate Cancer Prostatic Dis. 2002;5(2):88-95. To Reference
Ref 5Overexpression of the alpha1B-adrenergic receptor causes apoptotic neurodegeneration: multiple system atrophy. Nat Med. 2000 Dec;6(12):1388-94. 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
Ref 8J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. To Reference
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
Ref 10Bioorg 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 11J 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
Ref 12J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors. To Reference
Ref 13J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors. To Reference
Ref 14J Med Chem. 1997 Sep 12;40(19):3014-24.Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket". To Reference
Ref 15J 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
Ref 16Bioorg Med Chem Lett. 2006 May 15;16(10):2786-90. Epub 2006 Mar 2.Vasorelaxant activity of phthalazinones and related compounds. To Reference
Ref 17J Med Chem. 2000 Mar 9;43(5):765-8.alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor. To Reference
Ref 18J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines. To Reference
Ref 19Bioorg Med Chem Lett. 2006 Jan 15;16(2):257-61. Epub 2005 Nov 3.Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids. To Reference
Ref 20J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. To Reference
Ref 21Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995) To Reference
Ref 22J 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 23J 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 24J 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 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. 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 29Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. To Reference
Ref 30J 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 31J 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 32J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. To Reference
Ref 33J 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 34J 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 35Daws 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



 

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