Target
Information |
Name | Neuronal acetylcholine receptor protein, beta-2 chain |
Type of target | Discontinued target |
Synonyms | Beta-2 nAChR |
Nicotinic acetylcholine receptor beta 2-subunit protein |
Nicotinic acetylcholine receptor beta2 |
Disease | Alzheimer'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-894 |  | Discontinued in Phase II completed | Neuropathic pain | [4][5] |
BioChemical Class | Ion transport |
UniProt ID | P17787 |
PDB Structure | 2GVT; 2K58; 2K59. |
Function | After 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. |
Sequence | MARRCGPVALLLGFGLLRLCSGVWGTDTEERLVEHLLDPSRYNKLIRPATNGSELVTVQL
MVSLAQLISVHEREQIMTTNVWLTQEWEDYRLTWKPEEFDNMKKVRLPSKHIWLPDVVLY
NNADGMYEVSFYSNAVVSYDGSIFWLPPAIYKSACKIEVKHFPFDQQNCTMKFRSWTYDR
TEIDLVLKSEVASLDDFTPSGEWDIVALPGRRNENPDDSTYVDITYDFIIRRKPLFYTIN
LIIPCVLITSLAILVFYLPSDCGEKMTLCISVLLALTVFLLLISKIVPPTSLDVPLVGKY
LMFTMVLVTFSIVTSVCVLNVHHRSPTTHTMAPWVKVVFLEKLPALLFMQQPRHHCARQR
LRLRRRQREREGAGALFFREAPGADSCTCFVNRASVQGLAGAFGAEPAPVAGPGRSGEPC
GCGLREAVDGVRFIADHMRSEDDDQSVSEDWKYVAMVIDRLFLWIFVFVCVFGTIGMFLQ
PLFQNYTTTTFLHSDHSAPSSK
|
Target Validation | Click 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] |
Agonist | ABT-418 |  | [1][14] |
ABT-594 |  | [3] |
ABT-894 |  | [4][5] |
SIB-1508Y |  | [1] |
Antagonist | Laudanosine |  | [15] |
Volatile anesthetics |  | [16] |
Binder | Nicotine replacement |  | [2] |
Multitarget | ABT-894 |  | [4][5] |
Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
Ref 1 | Nicotine, brain nicotinic receptors, and neuropsychiatric disorders. Arch Med Res. 2000 Mar-Apr;31(2):131-44. To Reference |
Ref 2 | Nicotine dependence--mechanisms and therapeutic strategies. Biochem Soc Symp. 1993;59:83-95. To Reference |
Ref 3 | The 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 4 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference |
Ref 5 | Modulators of nicotinic acetylcholine receptors as analgesics. Curr Opin Investig Drugs. 2004 Jan;5(1):76-81. To Reference |
Ref 6 | J 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 7 | Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6. Epub 2006 Jun 9.Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. To Reference |
Ref 8 | J 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 9 | J 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 10 | Bioorg 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 11 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. To Reference |
Ref 12 | J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. To Reference |
Ref 13 | Bioorg 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 15 | Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. To Reference |
Ref 16 | The role of nicotinic acetylcholine receptors in the mechanisms of anesthesia. Brain Res Bull. 2002 Jan 15;57(2):133-50. To Reference |