Target Information
Target General Infomation | |||||
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Target ID |
T78111
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Former ID |
TTDS00303
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Target Name |
Nicotinic acetylcholine receptor
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Synonyms |
Nicotinergic acetylcholine receptor; nAChR
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Target Type |
Successful
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Disease | Anesthesia [ICD9: 338; ICD10: R20.0] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
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
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Target Validation |
T78111
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Drugs and Mode of Action | |||||
Drug(s) | Atracurium | Drug Info | Approved | General anesthesia | [537821] |
Cotinine | Drug Info | Approved | Insecticide | [551871] | |
Mecamylamine | Drug Info | Approved | Moderately severe to severe essential hypertension | [551871] | |
Nicotine | Drug Info | Approved | Nicotine dependence | [538279], [539664] | |
Pancuronium | Drug Info | Approved | Anesthesia | [537286], [540618] | |
A-85380 | Drug Info | Phase 2 | Discovery agent | [521914], [540862] | |
Dexefaroxan | Drug Info | Phase 2 | Parkinson's disease | [526560] | |
TRIDMAC | Drug Info | Phase 2 | Severe mood disorders | [536580] | |
ATG002 | Drug Info | Phase 1/2 | Diabetic foot ulcer | [521825] | |
ABT-418 | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [545652] | |
ABT-594 | Drug Info | Discontinued in Phase 2 | Discovery agent | [540604], [546684] | |
Dexefaroxan | Drug Info | Discontinued in Phase 2 | Schizophrenia | [536463] | |
ORG-9273 | Drug Info | Discontinued in Phase 2 | Paralysis | [528223] | |
RJR-2403 | Drug Info | Discontinued in Phase 2 | Cognitive disorders | [540610], [546260] | |
SIB-1553A | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [546683] | |
ANQ-9040 | Drug Info | Discontinued in Phase 1 | Paralysis | [545509] | |
DBO-83 | Drug Info | Terminated | Discovery agent | [546586] | |
Dianicline+rimonabant | Drug Info | Terminated | Tobacco dependence | [548622] | |
SIB-1663 | Drug Info | Terminated | Discovery agent | [546105] | |
SIB-1765F | Drug Info | Terminated | Discovery agent | [546242] | |
Agonist | A-85380 | Drug Info | [535334] | ||
ABT-418 | Drug Info | [534879] | |||
ABT-594 | Drug Info | [534971], [538100] | |||
ATG002 | Drug Info | [551536] | |||
DBO-83 | Drug Info | [535334] | |||
Dexefaroxan | Drug Info | [536463] | |||
Dianicline+rimonabant | Drug Info | [537145] | |||
Epibatidine | Drug Info | [538102] | |||
RJR-2403 | Drug Info | [535334] | |||
SIB-1553A | Drug Info | [538102] | |||
SIB-1663 | Drug Info | [535334] | |||
SIB-1765F | Drug Info | [538011] | |||
Modulator | ANQ-9040 | Drug Info | [550884], [551871] | ||
Cotinine | Drug Info | [526328] | |||
ORG-9273 | Drug Info | [528223], [551871] | |||
Antagonist | Atracurium | Drug Info | [535185], [536169], [537286] | ||
Hexamethonium | Drug Info | [537877] | |||
Mecamylamine | Drug Info | [535489] | |||
Nicotine | Drug Info | [537393], [537394] | |||
Pancuronium | Drug Info | [537286] | |||
TRIDMAC | Drug Info | [536580] | |||
Inhibitor | PROTOSTEMODIOL | Drug Info | [529235] | ||
References | |||||
Ref 521825 | ClinicalTrials.gov (NCT00316537) Safety and Preliminary Efficacy Study of Nicotine Gel to Treat Diabetic Foot Ulcers. U.S. National Institutes of Health. | ||||
Ref 521914 | ClinicalTrials.gov (NCT00397696) Evaluation of 5-[123I]-A-85380 and SPECT Imaging in Individuals With Parkinsons Disease. U.S. National Institutes of Health. | ||||
Ref 526560 | Effects 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 528223 | Dose-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 536463 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 537286 | Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. | ||||
Ref 537821 | A preliminary assessment of atracurium, a new competitive neuromuscular blocking agent. Acta Anaesthesiol Scand. 1981 Feb;25(1):67-9. | ||||
Ref 538279 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074611. | ||||
Ref 539664 | (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 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 540610 | (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 540618 | (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 540862 | (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 545509 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003547) | ||||
Ref 545652 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004036) | ||||
Ref 546105 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006387) | ||||
Ref 546242 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007061) | ||||
Ref 546260 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007149) | ||||
Ref 546586 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009071) | ||||
Ref 546683 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009631) | ||||
Ref 546684 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009632) | ||||
Ref 526328 | Functional versus chemical diversity: is biodiversity important for drug discovery. Trends Pharmacol Sci. 2002 May;23(5):225-31. | ||||
Ref 528223 | Dose-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 529235 | J Nat Prod. 2008 Jan;71(1):112-6. Epub 2007 Dec 29.Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities. | ||||
Ref 534879 | Enhancement 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 534971 | The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13. | ||||
Ref 535185 | Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. | ||||
Ref 535334 | The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin Investig Drugs. 2001 Oct;10(10):1819-30. | ||||
Ref 535489 | Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7. | ||||
Ref 536463 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 537145 | Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. | ||||
Ref 537286 | Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. | ||||
Ref 537393 | Development 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 537394 | Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors. Neuropharmacology. 2009 Aug;57(2):183-91. Epub 2009 May 28. | ||||
Ref 537877 | Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ. 1994 Oct;5(10):1033-40. | ||||
Ref 538011 | Interactions 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 538100 | ABT-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. |
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