Target Information
Target General Infomation | |||||
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Target ID |
T63967
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Target Name |
Nicotinic ACh receptor alpha 4/beta 2
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Synonyms |
Nicotinic acetylcholine receptor alpha4/beta2
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Target Type |
Successful
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Disease | Anesthesia [ICD9: 338; ICD10: R20.0] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90] | |||||
Attention deficit hyperactivity disorder; Schizophrenia; Anxiety; Dementia [ICD9: 290-294, 295, 300, 314.0; ICD10: F01-F07, F20, F40-F42, 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] | |||||
Schizophrenia; Alzheimer disease [ICD9: 295, 331.0; ICD10: F20, G30] | |||||
Smoking cessation [ICD9: 292; ICD10: F17.2] | |||||
Tobacco dependence [ICD9: 305.1; ICD10: F17] | |||||
BioChemical Class |
Channels/Pores (TC=1)
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UniProt ID | |||||
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 522191 | ClinicalTrials.gov (NCT00583544) A Safety and Tolerability Single Ascending Dose Study in Healthy Volunteers. U.S. National Institutes of Health. | ||||
Ref 522853 | ClinicalTrials.gov (NCT01012375) Study to Investigate the Efficacy and Tolerability of AZD1446 in Adult ADHD Patients.. U.S. National Institutes of Health. | ||||
Ref 522995 | ClinicalTrials.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 523082 | ClinicalTrials.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 525768 | Recombinant 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 529637 | Pharmacological 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 532857 | Sofinicline: 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 536499 | Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. | ||||
Ref 537145 | Emerging 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 546915 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011083) | ||||
Ref 547885 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020139) | ||||
Ref 531488 | Toxicity 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 531558 | Antinociceptive 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 532306 | alpha4beta2 Nicotinic receptors play a role in the nAChR-mediated decline in L-dopa-induced dyskinesias in parkinsonian rats. Neuropharmacology. 2013 Aug;71:191-203. |
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