Target Information

Target General Infomation
Target ID
T63967
Target Name
Nicotinic ACh receptor alpha 4/beta 2
Synonyms
Nicotinic acetylcholine receptor alpha4/beta2
Target Type
Successful
Disease Attention deficit hyperactivity disorder; Schizophrenia; Anxiety; Dementia [ICD9: 290-294, 295, 300, 314.0; ICD10: F01-F07, F20, F40-F42, F90]
Anesthesia [ICD9: 338; ICD10: R20.0]
Alzheimer disease [ICD9: 331; ICD10: G30]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Gastrointestinal disease [ICD10: K00-K93]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Mood disorder [ICD10: F30-F39]
Parkinson's disease [ICD9: 332; ICD10: G20]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Smoking cessation [ICD9: 292; ICD10: F17.2]
Schizophrenia; Alzheimer disease [ICD9: 295, 331.0; ICD10: F20, G30]
Tobacco dependence [ICD9: 305.1; ICD10: F17]
BioChemical Class
Channels/Pores (TC=1)
UniProt ID
P43681||P17787
Drugs and Mode of Action
Drug(s) Metocurine Iodide Drug Info Approved Anesthesia [550733]
Varenicline Drug Info Approved Smoking cessation [528715], [540860]
AZD-1446 Drug Info Phase 2 Alzheimer disease [522853]
CP-601927 Drug Info Phase 2 Gastrointestinal disease [522995]
Sofinicline Drug Info Phase 2 Attention deficit hyperactivity disorder [532857]
TC-6499-12 Drug Info Phase 2 Irritable bowel syndrome [523082]
TC-2216 Drug Info Phase 1 Mood disorder [522191]
A-366833 Drug Info Preclinical Pain [547885]
Dianicline Drug Info Discontinued in Phase 3 Tobacco dependence [537145]
ABT-089 Drug Info Discontinued in Phase 2 Attention deficit hyperactivity disorder; Schizophrenia; Anxiety; Dementia [536499]
Ispronicline Drug Info Discontinued in Phase 2 Schizophrenia; Alzheimer disease [546915]
TC-2696 Drug Info Discontinued in Phase 2 Pain [547992]
SIB-1508Y Drug Info Terminated Parkinson's disease [525768], [529637]
Modulator A-366833 Drug Info [531558]
ABT-089 Drug Info
AZD-1446 Drug Info
CP-601927 Drug Info [531488]
Dianicline Drug Info
Ispronicline Drug Info
Metocurine Iodide Drug Info
SIB-1508Y Drug Info
Sofinicline Drug Info [532857]
TC-2216 Drug Info
TC-2696 Drug Info [532306]
TC-6499-12 Drug Info [1572591]
Varenicline Drug Info [528715]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
Ref 522191ClinicalTrials.gov (NCT00583544) A Safety and Tolerability Single Ascending Dose Study in Healthy Volunteers. U.S. National Institutes of Health.
Ref 522853ClinicalTrials.gov (NCT01012375) Study to Investigate the Efficacy and Tolerability of AZD1446 in Adult ADHD Patients.. U.S. National Institutes of Health.
Ref 522995ClinicalTrials.gov (NCT01098240) A Study Of The Efficacy And Safety Of CP-601,927 Augmentation Of Antidepressant Therapy In Major Depression. U.S. National Institutes of Health.
Ref 523082ClinicalTrials.gov (NCT01149200) Proof-of-Principle Study of TC-6499 in the Treatment of Constipation Predominant Irritable Bowel Syndrome (IBS). U.S. National Institutes of Health.
Ref 525768Recombinant human receptors and functional assays in the discovery of altinicline (SIB-1508Y), a novel acetylcholine-gated ion channel (nAChR) agonist. Pharm Acta Helv. 2000 Mar;74(2-3):125-30.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 529637Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist. Brain Res. 2008 Oct 9;1234:16-24.
Ref 532857Sofinicline: a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder. Expert Opin Investig Drugs. 2014 Aug;23(8):1157-63.
Ref 536499Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34.
Ref 537145Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32.
Ref 540860(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: 5459).
Ref 546915Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011083)
Ref 547885Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020139)
Ref 547992Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021012)
Ref 550733Drug information of Metocurine Iodide, 2008. eduDrugs.
Ref
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 531488Toxicity study in juvenile rats with the alpha4beta2 nicotinic acetylcholine receptor partial agonist CP-601,927. Birth Defects Res B Dev Reprod Toxicol. 2011 Aug;92(4):323-32.
Ref 531558Antinociceptive activity of alpha4beta2* neuronal nicotinic receptor agonist A-366833 in experimental models of neuropathic and inflammatory pain. Eur J Pharmacol. 2011 Oct 1;668(1-2):155-62.
Ref 532306alpha4beta2 Nicotinic receptors play a role in the nAChR-mediated decline in L-dopa-induced dyskinesias in parkinsonian rats. Neuropharmacology. 2013 Aug;71:191-203.
Ref 532857Sofinicline: a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder. Expert Opin Investig Drugs. 2014 Aug;23(8):1157-63.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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