Therapeutic Targets Database
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TTD Target ID: TTDC00301

Target Information
NameNeuronal acetylcholine receptor protein, beta-2 chain    
Type of targetDiscontinued target    
SynonymsBeta-2 nAChR    
Nicotinic acetylcholine receptor beta 2-subunit protein    
Nicotinic acetylcholine receptor beta2    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[1]
Analgesics
[ICD9: 338   ICD10: R52]
[1]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
[2]
Frontal lobe epilepsy
[ICD9: 345   ICD10: G40]
[1]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[3]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[1]
Drug(s)ABT-894Discontinued in Phase II completedNeuropathic pain[4][5]
BioChemical ClassIon transport    
UniProt IDP17787
PDB Structure2GVT; 2K58; 2K59.    
FunctionAfter binding acetylcholine, the achr responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.    
SequenceMARRCGPVALLLGFGLLRLCSGVWGTDTEERLVEHLLDPSRYNKLIRPATNGSELVTVQL MVSLAQLISVHEREQIMTTNVWLTQEWEDYRLTWKPEEFDNMKKVRLPSKHIWLPDVVLY NNADGMYEVSFYSNAVVSYDGSIFWLPPAIYKSACKIEVKHFPFDQQNCTMKFRSWTYDR TEIDLVLKSEVASLDDFTPSGEWDIVALPGRRNENPDDSTYVDITYDFIIRRKPLFYTIN LIIPCVLITSLAILVFYLPSDCGEKMTLCISVLLALTVFLLLISKIVPPTSLDVPLVGKY LMFTMVLVTFSIVTSVCVLNVHHRSPTTHTMAPWVKVVFLEKLPALLFMQQPRHHCARQR LRLRRRQREREGAGALFFREAPGADSCTCFVNRASVQGLAGAFGAEPAPVAGPGRSGEPC GCGLREAVDGVRFIADHMRSEDDDQSVSEDWKYVAMVIDRLFLWIFVFVCVFGTIGMFLQ PLFQNYTTTTFLHSDHSAPSSK
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2S,3S)-2-[6]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol[6]
3-[2- (N,N,N-trimethylammonium)ethoxy]pyridine[7]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[8]
6'-methylepibatidine[9]
BOLDINE[10]
CMI-489[9]
CYTISINE[11]
GCCSHPACAGNNQHIC*[12]
GCCSNPVCHLEHSNLC*[12]
HOMOEPIBATIDINE[11]
N,N-dimethyl (pyridin-3-yl)methanamine[13]
N,N-dimethyl-2- (pyridin-3-yloxy)ethanamine[13]
N,N-dimethyl-4- (pyridin-3-yl)but-3-yn-1-amine[13]
N-ethyl-N-methyl-4- (pyridin-3-yl)but-3-yn-1-amine[13]
N-methyl-2- (pyridin-3-yloxy)ethanamine[13]
N-methyl-4- (pyridin-3-yl)but-3-yn-1-amine[13]
N-methyl-N- (pyridin-3-ylmethyl)ethanamine[13]
N-methyllaurotetanine methiodide[10]
boldine methiodide[10]
glaucine methiodide[10]
predicentrine methiodide[10]
AgonistABT-418[1][14]
ABT-594[3]
ABT-894[4][5]
SIB-1508Y[1]
AntagonistLaudanosine[15]
Volatile anesthetics[16]
BinderNicotine replacement[2]
MultitargetABT-894[4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Nicotine, brain nicotinic receptors, and neuropsychiatric disorders. Arch Med Res. 2000 Mar-Apr;31(2):131-44. To Reference
Ref 2Nicotine dependence--mechanisms and therapeutic strategies. Biochem Soc Symp. 1993;59:83-95. To Reference
Ref 3The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13. To Reference
Ref 4Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 5Modulators of nicotinic acetylcholine receptors as analgesics. Curr Opin Investig Drugs. 2004 Jan;5(1):76-81. To Reference
Ref 6J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. To Reference
Ref 7Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6. Epub 2006 Jun 9.Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. To Reference
Ref 8J 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 9J Med Chem. 2007 Dec 13;50(25):6383-91. Epub 2007 Nov 10.Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine. To Reference
Ref 10Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. To Reference
Ref 11Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. To Reference
Ref 12J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. To Reference
Ref 13Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. To Reference
Ref 14(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization. J Pharmacol Exp Ther. 1994 Jul;270(1):319-28. To Reference
Ref 15Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. To Reference
Ref 16The role of nicotinic acetylcholine receptors in the mechanisms of anesthesia. Brain Res Bull. 2002 Jan 15;57(2):133-50. To Reference



 

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