Target Information

Target General Infomation
Target ID
T82543
Former ID
TTDC00301
Target Name
Neuronal acetylcholine receptor protein, beta-2 chain
Gene Name
CHRNB2
Synonyms
Beta-2 nAChR; Nicotinic acetylcholine receptor beta 2-subunit protein; Nicotinic acetylcholine receptor beta2; Alpha-4/beta-2 nicotinic receptor; CHRNB2
Target Type
Discontinued
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
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 permeable to sodiun ions.
BioChemical Class
Neurotransmitter receptor
Target Validation
T82543
UniProt ID
P17787
Sequence
MARRCGPVALLLGFGLLRLCSGVWGTDTEERLVEHLLDPSRYNKLIRPATNGSELVTVQL
MVSLAQLISVHEREQIMTTNVWLTQEWEDYRLTWKPEEFDNMKKVRLPSKHIWLPDVVLY
NNADGMYEVSFYSNAVVSYDGSIFWLPPAIYKSACKIEVKHFPFDQQNCTMKFRSWTYDR
TEIDLVLKSEVASLDDFTPSGEWDIVALPGRRNENPDDSTYVDITYDFIIRRKPLFYTIN
LIIPCVLITSLAILVFYLPSDCGEKMTLCISVLLALTVFLLLISKIVPPTSLDVPLVGKY
LMFTMVLVTFSIVTSVCVLNVHHRSPTTHTMAPWVKVVFLEKLPALLFMQQPRHHCARQR
LRLRRRQREREGAGALFFREAPGADSCTCFVNRASVQGLAGAFGAEPAPVAGPGRSGEPC
GCGLREAVDGVRFIADHMRSEDDDQSVSEDWKYVAMVIDRLFLWIFVFVCVFGTIGMFLQ
PLFQNYTTTTFLHSDHSAPSSK
Structure
2GVT; 2LLY; 2GVT; 2K58; 2K59; 2KSR; 2LM2
Drugs and Mode of Action
Drug(s) ABT-418 Drug Info Discontinued in Phase 2 Alzheimer disease [545652]
ABT-594 Drug Info Discontinued in Phase 2 Discovery agent [540604], [546684]
HOMOEPIBATIDINE Drug Info Terminated Discovery agent [546333]
Inhibitor (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info [530946]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info [530946]
3-[2-(N,N,N-trimethylammonium)ethoxy]pyridine Drug Info [528245]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
6'-methylepibatidine Drug Info [529145]
BOLDINE Drug Info [528761]
CMI-489 Drug Info [529145]
CYTISINE Drug Info [528394]
GCCSHPACAGNNQHIC* Drug Info [527644]
GCCSNPVCHLEHSNLC* Drug Info [527644]
HOMOEPIBATIDINE Drug Info [528394]
N,N-dimethyl(pyridin-3-yl)methanamine Drug Info [527965]
N,N-dimethyl-2-(pyridin-3-yloxy)ethanamine Drug Info [527965]
N,N-dimethyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info [527965]
N-ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info [527965]
N-methyl-2-(pyridin-3-yloxy)ethanamine Drug Info [527965]
N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info [527965]
N-methyl-N-(pyridin-3-ylmethyl)ethanamine Drug Info [527965]
Predicentrine methiodide Drug Info [528761]
Blocker (channel blocker) A-867744 Drug Info [530093]
NS1738 Drug Info [528946]
Agonist ABT-418 Drug Info [535007], [537889]
ABT-594 Drug Info [534971]
TC-2559 Drug Info [526677]
[125I]epibatidine Drug Info [543842]
[3H]cytisine Drug Info [543842]
[3H]epibatidine Drug Info [543842]
[3H]nicotine Drug Info [543842]
Antagonist Laudanosine Drug Info [535185]
Volatile anesthetics Drug Info [535371]
Modulator (allosteric modulator) LY2087101 Drug Info [528221]
NS9283 Drug Info [531561]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Cholinergic synapse
Nicotine addiction
PANTHER Pathway Nicotinic acetylcholine receptor signaling pathway
Nicotine pharmacodynamics pathway
Reactome Highly sodium permeable acetylcholine nicotinic receptors
Highly calcium permeable postsynaptic nicotinic acetylcholine receptors
Highly calcium permeable nicotinic acetylcholine receptors
WikiPathways SIDS Susceptibility Pathways
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Nicotine Activity on Dopaminergic Neurons
References
Ref 540604(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3989).
Ref 545652Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004036)
Ref 546333Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007531)
Ref 546684Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009632)
Ref 526677The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices. Neuropharmacology. 2003 Sep;45(3):334-44.
Ref 527644J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Ref 527965Bioorg 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.
Ref 528221Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators. J Pharmacol Exp Ther. 2006 Sep;318(3):1108-17. Epub 2006 May 31.
Ref 528245Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6. Epub 2006 Jun 9.Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
Ref 528394Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships.
Ref 528761Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
Ref 528946An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307. Epub 2007 Jul 11.
Ref 529145J 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.
Ref 530093J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. Epub 2009 Apr 23.In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Ref 530946J 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.
Ref 531079J 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.
Ref 531561alpha4beta2 neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of alpha4beta2 nAChR agonists in pain. Biochem Pharmacol. 2011 Oct 15;82(8):959-66.
Ref 534971The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13.
Ref 535007Nicotine, brain nicotinic receptors, and neuropsychiatric disorders. Arch Med Res. 2000 Mar-Apr;31(2):131-44.
Ref 535185Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51.
Ref 535371The role of nicotinic acetylcholine receptors in the mechanisms of anesthesia. Brain Res Bull. 2002 Jan 15;57(2):133-50.
Ref 537889(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.
Ref 543842(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 465).

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