Therapeutic Targets Database
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TTD Target ID: TTDS00029

Target Information
NameAlpha-1B adrenergic receptor    
Type of targetSuccessful target    
SynonymsAlpha 1B-adrenoceptor    
Alpha 1B-adrenoreceptor    
DiseaseShy-Drager syndrome[1]
Drug(s)DextroamphetamineApprovedAttention deficit hyperactivity disorder[2]
LisdexamfetamineApprovedAttention deficit hyperactivity disorder[2]
MethamphetamineApprovedAttention deficit hyperactivity disorder[3]
MethoxamineApprovedHypertension[4]
PhendimetrazineApprovedObesity[2]
PropericiazineApprovedPsychotic disorders[5]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP35368
FunctionThis alpha-adrenergic receptor mediates its action by association with g proteins that activate a phosphatidylinositol-calcium second messenger system.    
SequenceMNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
Related US Patent6,303,606
6,559,153
6,642,228
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[6]
(2,6-Dichloro-phenyl)-[7]
(2-Bromo-phenyl)-[7]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline[8]
4- ([9]
4- ([9]
4- (1-Naphthalen-1-yl-ethyl)-1H-imidazole[10]
4- (1-Naphthalen-1-yl-propyl)-1H-imidazole[9]
4- (1-Naphthalen-1-yl-vinyl)-1H-imidazole[9]
4- (2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole[9]
4- (3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline[8]
4- (3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol[11]
4- (4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol[11]
4- (4-Methyl-indan-1-yl)-1H-imidazole[12]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[13]
4-Benzo[b]thiophen-4-yl-1H-imidazole[14]
4-Morpholin-2-yl-benzene-1,2-diol[11]
6-fluoronorepinehprine[15]
A-119637[16]
A-123189[16]
ABANOQUIL[17]
AGN-192172[18]
AGN-193080[18]
BMY-7378[19]
CORYNANTHEINE[20]
FLUANISONE[21]
ISOCLOZAPINE[22]
Imidazolidin-2-ylidene-o-tolyl-amine[18]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine[18]
LEVONORDEFRIN[9]
MAZAPERTINE[23]
MEDETOMIDINE[10]
N- (5-Bromo-quinoxalin-6-yl)-guanidine[18]
NIGULDIPINE[20]
OCTOCLOTHEPIN[24]
RWJ-25730[23]
RWJ-68157[25]
RWJ-69736[25]
RX-821002[26]
SK&F-104078,   SK-104078[20]
SK&F-104856,   SK-104856[20]
SK&F-105854,   SK-105854[20]
SK&F-106686,   SK-106686[20]
SK&F-86466,   SK-86466[20]
SNAP-5089[20]
SNAP-8719[19]
Siramesine[27]
TIOSPIRONE[28]
UH-301[29]
WAY-100135[29]
WB-4101[17]
sunepitron[30]
AntagonistCyclazosin[31]
Dextroamphetamine[2]
Lisdexamfetamine[2]
Methamphetamine[3]
Phendimetrazine[2]
StimulatorMethoxamine[4]
BinderPropericiazine[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Overexpression of the alpha1B-adrenergic receptor causes apoptotic neurodegeneration: multiple system atrophy. Nat Med. 2000 Dec;6(12):1388-94. To Reference
Ref 2Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 3Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9. Epub 2008 Oct 21. To Reference
Ref 4Activation of alpha1-adrenoceptors Inhibits Growth Hormone Secretion in Humans. Exp Clin Endocrinol Diabetes. 2009 Apr 16. [Epub ahead of print] To Reference
Ref 5Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. 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 8Bioorg 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 9J 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 10J 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 11J 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 12J 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 13J 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 14J 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 15Bioorg Med Chem. 2009 Dec 1;17(23):7987-92. Epub 2009 Oct 13.Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. To Reference
Ref 16Bioorg Med Chem Lett. 2001 May 7;11(9):1119-21.Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. To Reference
Ref 17J 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 18Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995) To Reference
Ref 19J 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 20J 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 21J 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 22J 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 23J 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 24J 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 25Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. To Reference
Ref 26J 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 27J 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 28J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. To Reference
Ref 29J 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 30J 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 31Identification of alpha1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens. Eur J Pharmacol. 2009 Jan 14;602(2-3):388-94. Epub 2008 Nov 14. To Reference



 

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