Therapeutic Targets Database
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TTD Target ID: TTDC00293

Target Information
NameAlpha-2B adrenergic receptor    
Type of targetClinical trial target    
SynonymsAlpha-2B adrenoceptor    
Alpha-2B adrenoreceptor    
Subtype C2    
DiseaseHeart failure    [1]
Hypertension    [1]
Ischemic heart disease    [1]
Drug(s)AGN-199981Phase IINeuropathic pain[2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP18089
PDB Structure2CVA.    
FunctionAlpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline.    
SequenceMDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADIL VATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEY NSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGS FFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASV ASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEE EEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRR AQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSS LNPVIYTIFNQDFRRAFRRILCRPWTQTAW
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[3]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol[4]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine[5]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine[5]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine[5]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline[6]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline[6]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl[7]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline[8]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine[6]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol[9]
1,2,3,4-Tetrahydro-isoquinolin-7-ol[9]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole[10]
1,2,3,4-tetrahydroisoquinoline[11]
1- (3-Fluoro-pyridin-2-yl)-4-methyl-piperazine[7]
1-Pyridin-2-yl-piperazine[7]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine[6]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine[6]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine[6]
2,3-Dihydro-1H-isoindole[6]
2-Benzofuran-2-yl-4,5-dihydro-1H-imidazole[12]
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline[13]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline[4]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline[6]
4- (1-Naphthalen-1-yl-ethyl)-1H-imidazole[14]
4- (4-Methyl-indan-1-yl)-1H-imidazole[15]
4-Benzo[b]thiophen-4-yl-1H-imidazole[16]
5-Aminomethyl-naphthalen-2-ol[9]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene[6]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline[17]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline[9]
A-80426[18]
Butyl-indol-1-yl-pyridin-4-yl-amine[5]
C- (6-Methoxy-naphthalen-1-yl)-methylamine[9]
C-Naphthalen-1-yl-methylamine[9]
Ethyl-indol-1-yl-pyridin-4-yl-amine[5]
GNF-PF-2857[19]
GNF-PF-3427[19]
GNF-PF-3878[19]
INDORAMIN[20]
Indol-1-yl-methyl-pyridin-4-yl-amine[5]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine[5]
Indol-1-yl-propyl-pyridin-4-yl-amine[5]
Indol-1-yl-pyridin-4-yl-amine[5]
MAZAPERTINE[21]
MEDETOMIDINE[14]
METHYLNORADRENALINE[22]
MEZILAMINE[23]
MOXONIDINE[24]
PIPEROXAN[22]
R-226161[25]
RX-821002[26]
S-34324[18]
SK&F-104078,   SK-104078[20]
SK&F-64139,   SK-64139[11]
SNAP-5089[27]
SNAP-5150[27]
TRACIZOLINE[17]
TRAMAZOLINE[22]
TRYPTOLINE[17]
WB-4101[22]
AgonistAGN-199981[2]
AntagonistARC-239[28][29]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The alpha2 -adrenergic receptors in hypertension and heart failure: experimental and clinical studies. J Hypertens. 2001 Dec;19(12):2115-24. To Reference
Ref 2Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 3Bioorg 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 4J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor. To Reference
Ref 5J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. To Reference
Ref 6J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase. To Reference
Ref 7J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines. To Reference
Ref 8J Med Chem. 1998 Oct 8;41(21):4165-70.N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies. To Reference
Ref 9J Med Chem. 1997 Dec 5;40(25):3997-4005.Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. To Reference
Ref 10Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands. To Reference
Ref 11J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase. To Reference
Ref 12Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7.Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand. To Reference
Ref 13J Med Chem. 2005 Jan 13;48(1):134-40.3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. To Reference
Ref 14J 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 15J 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 16J 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 17Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors. To Reference
Ref 18J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. To Reference
Ref 19J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists. 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 21J 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 22J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs. To Reference
Ref 23J Med Chem. 1986 Aug;29(8):1394-8.4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors. To Reference
Ref 24J Med Chem. 1996 Mar 15;39(6):1193-5.Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. To Reference
Ref 25Bioorg 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 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 27Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.Design and synthesis of novel dihydropyridine alpha-1a antagonists. To Reference
Ref 28Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. To Reference
Ref 29Silent alpha(2C)-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries. Am J Physiol Heart Circ Physiol. 2000 Apr;278(4):H1075-83. To Reference



 

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