Target Information

Target General Infomation
Target ID
T78111
Former ID
TTDS00303
Target Name
Nicotinic acetylcholine receptor
Synonyms
Nicotinergic acetylcholine receptor; nAChR
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Anesthesia [ICD9: 338; ICD10: R20.0]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89]
General anesthesia [ICD9: 338; ICD10: R20.0]
Insecticide [ICD10: F19.20]
Moderately severe to severe essential hypertension [ICD10: I10]
Nicotine dependence [ICD9: 305.1; ICD10: F17]
Parkinson's disease [ICD9: 332; ICD10: G20]
Paralysis [ICD10: G72.3]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Schizophrenia [ICD9: 295; ICD10: F20]
Tobacco dependence [ICD9: 305.1; ICD10: F17]
BioChemical Class
Ion transport
Target Validation
T78111
Drugs and Mode of Action
Drug(s) Atracurium Drug Info Approved General anesthesia [1]
Cotinine Drug Info Approved Insecticide [2]
Mecamylamine Drug Info Approved Moderately severe to severe essential hypertension [2]
Nicotine Drug Info Approved Nicotine dependence [3], [4]
Pancuronium Drug Info Approved Anesthesia [5], [6]
A-85380 Drug Info Phase 2 Discovery agent [7], [8]
Dexefaroxan Drug Info Phase 2 Parkinson's disease [9]
TRIDMAC Drug Info Phase 2 Severe mood disorders [10]
ATG002 Drug Info Phase 1/2 Diabetic foot ulcer [11]
ABT-418 Drug Info Discontinued in Phase 2 Alzheimer disease [12]
ABT-594 Drug Info Discontinued in Phase 2 Discovery agent [13], [14]
Dexefaroxan Drug Info Discontinued in Phase 2 Schizophrenia [15]
ORG-9273 Drug Info Discontinued in Phase 2 Paralysis [16]
RJR-2403 Drug Info Discontinued in Phase 2 Cognitive disorders [17], [18]
SIB-1553A Drug Info Discontinued in Phase 2 Alzheimer disease [19]
ANQ-9040 Drug Info Discontinued in Phase 1 Paralysis [20]
DBO-83 Drug Info Terminated Discovery agent [21]
Dianicline+rimonabant Drug Info Terminated Tobacco dependence [22]
SIB-1663 Drug Info Terminated Discovery agent [23]
SIB-1765F Drug Info Terminated Discovery agent [24]
Agonist A-85380 Drug Info [25]
ABT-418 Drug Info [26]
ABT-594 Drug Info [27], [28]
ATG002 Drug Info [29]
DBO-83 Drug Info [25]
Dexefaroxan Drug Info [15]
Dianicline+rimonabant Drug Info [30]
Epibatidine Drug Info [31]
RJR-2403 Drug Info [25]
SIB-1553A Drug Info [31]
SIB-1663 Drug Info [25]
SIB-1765F Drug Info [32]
Modulator ANQ-9040 Drug Info [33], [2]
Cotinine Drug Info [34]
ORG-9273 Drug Info [16], [2]
Antagonist Atracurium Drug Info [35], [36], [5]
Hexamethonium Drug Info [37]
Mecamylamine Drug Info [38]
Nicotine Drug Info [39], [40]
Pancuronium Drug Info [5]
TRIDMAC Drug Info [10]
Inhibitor PROTOSTEMODIOL Drug Info [41]
References
REF 1A preliminary assessment of atracurium, a new competitive neuromuscular blocking agent. Acta Anaesthesiol Scand. 1981 Feb;25(1):67-9.
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074611.
REF 4(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: 2585).
REF 5Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52.
REF 6(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: 4001).
REF 7ClinicalTrials.gov (NCT00397696) Evaluation of 5-[123I]-A-85380 and SPECT Imaging in Individuals With Parkinsons Disease. U.S. National Institutes of Health.
REF 8(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: 5460).
REF 9Effects of the alpha 2-adrenoreceptor antagonist dexefaroxan on neurogenesis in the olfactory bulb of the adult rat in vivo: selective protection against neuronal death. Neuroscience. 2003;117(2):281-91.
REF 10Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 11ClinicalTrials.gov (NCT00316537) Safety and Preliminary Efficacy Study of Nicotine Gel to Treat Diabetic Foot Ulcers. U.S. National Institutes of Health.
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004036)
REF 13(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 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009632)
REF 15The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
REF 16Dose-response relation, neuromuscular blocking action, intubation conditions, and cardiovascular effects of Org 9273, a new neuromuscular blocking agent. Anesth Analg. 1991 Jun;72(6):811-6.
REF 17(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: 3994).
REF 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007149)
REF 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009631)
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003547)
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009071)
REF 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143)
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006387)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007061)
REF 25The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin Investig Drugs. 2001 Oct;10(10):1819-30.
REF 26Enhancement of sustained attention performance by the nicotinic acetylcholine receptor agonist ABT-418 in intact but not basal forebrain-lesioned rats. Psychopharmacology (Berl). 1999 May;144(2):175-82.
REF 27The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13.
REF 28ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization. J Pharmacol Exp Ther. 1998 May;285(2):787-94.
REF 29Athenagen Advances Angiogenesis Drug to Clinical Testing. Athenagen. JUNE 21, 2006.
REF 30Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32.
REF 31The potential of subtype-selective neuronal nicotinic acetylcholine receptor agonists as therapeutic agents. Life Sci. 1998;62(17-18):1601-6.
REF 32Interactions between a novel cholinergic ion channel agonist, SIB-1765F and L-DOPA in the reserpine model of Parkinson's disease in rats. J Pharmacol Exp Ther. 1997 Jan;280(1):393-401.
REF 33Patent US20030087306 A1.
REF 34Functional versus chemical diversity: is biodiversity important for drug discovery. Trends Pharmacol Sci. 2002 May;23(5):225-31.
REF 35Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51.
REF 36Neuromuscular block. Br J Pharmacol. 2006 Jan;147 Suppl 1:S277-86.
REF 37Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ. 1994 Oct;5(10):1033-40.
REF 38Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7.
REF 39Development and optimization of a high-throughput electrophysiology assay for neuronal alpha4beta2 nicotinic receptors. J Neurosci Methods. 2009 Aug 30;182(1):17-24. Epub 2009 May 27.
REF 40Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors. Neuropharmacology. 2009 Aug;57(2):183-91. Epub 2009 May 28.
REF 41J Nat Prod. 2008 Jan;71(1):112-6. Epub 2007 Dec 29.Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities.

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