Target Information
Target General Information | Top | |||||
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Target ID |
T78111
(Former ID: TTDS00303)
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Target Name |
Nicotinic acetylcholine receptor (nAChR)
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Synonyms |
nAChR; Nicotinergic acetylcholine receptor
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Gene Name |
NO-GeName
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 4 Target-related Diseases | + | ||||
1 | Corneal disease [ICD-11: 9A76-9A78] | |||||
2 | Essential hypertension [ICD-11: BA00] | |||||
3 | Insecticide [ICD-11: N.A.] | |||||
4 | Nicotine use disorder [ICD-11: 6C4A] | |||||
Function |
After binding acetylcholine, the AChRresponds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
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BioChemical Class |
Ion transport
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UniProt ID |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 5 Approved Drugs | + | ||||
1 | Atracurium | Drug Info | Approved | Anaesthesia | [2] | |
2 | Cotinine | Drug Info | Approved | Insecticide | [3] | |
3 | Mecamylamine | Drug Info | Approved | Essential hypertension | [3] | |
4 | Nicotine | Drug Info | Approved | Nicotine dependence | [4], [5] | |
5 | Pancuronium | Drug Info | Approved | Anaesthesia | [6], [7] | |
Clinical Trial Drug(s) | [+] 11 Clinical Trial Drugs | + | ||||
1 | CYTISINE | Drug Info | Phase 3 | Tobacco dependence | [8] | |
2 | ASM-024 | Drug Info | Phase 2 | Asthma | [9] | |
3 | BMS-954561 | Drug Info | Phase 2 | Diabetic neuropathy | [10] | |
4 | Dexefaroxan | Drug Info | Phase 2 | Parkinson disease | [11] | |
5 | NIC-002 | Drug Info | Phase 2 | Nicotine dependence | [12] | |
6 | TRIDMAC | Drug Info | Phase 2 | Mood disorder | [13] | |
7 | ATG002 | Drug Info | Phase 1/2 | Diabetic foot ulcer | [14] | |
8 | GANTACURIUM CHLORIDE | Drug Info | Phase 1/2 | Anaesthesia | [15] | |
9 | ND-0801 | Drug Info | Phase 1/2 | Attention deficit hyperactivity disorder | [16] | |
10 | RPI-78M | Drug Info | Phase 1 | Multiple sclerosis | [17], [18] | |
11 | RPI-MN | Drug Info | Phase 1 | Amyotrophic lateral sclerosis | [18] | |
Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
1 | Inaperisone | Drug Info | Discontinued in Preregistration | Pollakiuria | [19] | |
2 | ABT-418 | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [20] | |
3 | ORG-9273 | Drug Info | Discontinued in Phase 2 | Paralysis | [21] | |
4 | RJR-2403 | Drug Info | Discontinued in Phase 2 | Cognitive impairment | [22], [23] | |
5 | SIB-1553A | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [24] | |
6 | ABT-202 | Drug Info | Discontinued in Phase 1 | Pain | [25] | |
7 | ANQ-9040 | Drug Info | Discontinued in Phase 1 | Paralysis | [26] | |
8 | Dianicline+rimonabant | Drug Info | Terminated | Tobacco dependence | [27] | |
9 | NNC-90-0270 | Drug Info | Terminated | Alzheimer disease | [28] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Antagonist | [+] 9 Antagonist drugs | + | ||||
1 | Atracurium | Drug Info | [7], [29], [30] | |||
2 | Mecamylamine | Drug Info | [1] | |||
3 | Nicotine | Drug Info | [32], [33] | |||
4 | Pancuronium | Drug Info | [7] | |||
5 | CYTISINE | Drug Info | [8] | |||
6 | TRIDMAC | Drug Info | [13] | |||
7 | RPI-78M | Drug Info | [17], [18] | |||
8 | RPI-MN | Drug Info | [18] | |||
9 | 8-aminoquinolines | Drug Info | [51] | |||
Modulator | [+] 8 Modulator drugs | + | ||||
1 | Cotinine | Drug Info | [31] | |||
2 | BMS-954561 | Drug Info | [36] | |||
3 | GANTACURIUM CHLORIDE | Drug Info | [40] | |||
4 | ND-0801 | Drug Info | [41] | |||
5 | Inaperisone | Drug Info | [42] | |||
6 | ORG-9273 | Drug Info | [21], [3] | |||
7 | ABT-202 | Drug Info | [47] | |||
8 | ANQ-9040 | Drug Info | [48], [3] | |||
Agonist | [+] 14 Agonist drugs | + | ||||
1 | A-85380 | Drug Info | [34] | |||
2 | ASM-024 | Drug Info | [35] | |||
3 | Dexefaroxan | Drug Info | [37] | |||
4 | ATG002 | Drug Info | [39] | |||
5 | ABT-418 | Drug Info | [43] | |||
6 | ABT-594 | Drug Info | [44], [45] | |||
7 | RJR-2403 | Drug Info | [34] | |||
8 | SIB-1553A | Drug Info | [46] | |||
9 | DBO-83 | Drug Info | [34] | |||
10 | Dianicline+rimonabant | Drug Info | [49] | |||
11 | NNC-90-0270 | Drug Info | [28] | |||
12 | SIB-1663 | Drug Info | [34] | |||
13 | SIB-1765F | Drug Info | [50] | |||
14 | Epibatidine | Drug Info | [46] | |||
Inhibitor | [+] 1 Inhibitor drugs | + | ||||
1 | PROTOSTEMODIOL | Drug Info | [52] |
Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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REF 1 | Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7. | |||||
REF 2 | A preliminary assessment of atracurium, a new competitive neuromuscular blocking agent. Acta Anaesthesiol Scand. 1981 Feb;25(1):67-9. | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 4 | URL: 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 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074611. | |||||
REF 6 | URL: 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 7 | 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 8 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 9 | ClinicalTrials.gov (NCT01190826) Safety, Tolerability and Clinical Activity of ASM-024 in Stable Moderate Asthma. U.S. National Institutes of Health. | |||||
REF 10 | ClinicalTrials.gov (NCT01314222) Diabetic Peripheral Neuropathic Pain (DPNP). U.S. National Institutes of Health. | |||||
REF 11 | 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 12 | ClinicalTrials.gov (NCT00369616) Efficacy and Safety of Nicotine-Qbeta Vaccine in Smokers. U.S. National Institutes of Health. | |||||
REF 13 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. | |||||
REF 14 | ClinicalTrials.gov (NCT00316537) Safety and Preliminary Efficacy Study of Nicotine Gel to Treat Diabetic Foot Ulcers. U.S. National Institutes of Health. | |||||
REF 15 | ClinicalTrials.gov (NCT00235976) The Efficacy and Safety of Gantacurium Chloride for Injection in Tracheal Intubation in Healthy Adult Patients Undergoing Surgery Under General Anesthesia. U.S. National Institutes of Health. | |||||
REF 16 | ClinicalTrials.gov (NCT01174355) A Study of ND0801 in Attention Deficit/Hyperactivity Disorder (ADHD). U.S. National Institutes of Health. | |||||
REF 17 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 18 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003120) | |||||
REF 20 | 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 21 | 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 22 | URL: 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 23 | 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 24 | 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 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015975) | |||||
REF 26 | 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 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143) | |||||
REF 28 | Nicotinic agonists, antagonists, and modulators from natural sources. Cell Mol Neurobiol. 2005 Jun;25(3-4):513-52. | |||||
REF 29 | Neuromuscular block. Br J Pharmacol. 2006 Jan;147 Suppl 1:S277-86. | |||||
REF 30 | Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. | |||||
REF 31 | Functional versus chemical diversity: is biodiversity important for drug discovery. Trends Pharmacol Sci. 2002 May;23(5):225-31. | |||||
REF 32 | Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors. Neuropharmacology. 2009 Aug;57(2):183-91. | |||||
REF 33 | Development and optimization of a high-throughput electrophysiology assay for neuronal alpha4beta2 nicotinic receptors. J Neurosci Methods. 2009 Aug 30;182(1):17-24. | |||||
REF 34 | The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin Investig Drugs. 2001 Oct;10(10):1819-30. | |||||
REF 35 | Effects of ASM-024, a modulator of acetylcholine receptor function, on airway responsiveness and allergen-induced responses in patients with mild asthma. Can Respir J. 2015 Jul-Aug;22(4):230-4. | |||||
REF 36 | EP patent application no. 2774991, Drug delivery system for use in the treatment or diagnosis of neurological disorders. | |||||
REF 37 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
REF 38 | Therapeutic advances in the treatment of nicotine addiction: present and future. Ther Adv Chronic Dis. 2010 May; 1(3): 95-106. | |||||
REF 39 | Athenagen Advances Angiogenesis Drug to Clinical Testing. Athenagen. JUNE 21, 2006. | |||||
REF 40 | Gantacurium and CW002 do not potentiate muscarinic receptor-mediated airway smooth muscle constriction in guinea pigs. Anesthesiology. 2010 April; 112(4): 892-899. | |||||
REF 41 | Drugs in Clinical Development for Attention-Deficit/Hyperactivity Disorder: Summary and Table, 2013, Volume 27, Issue 4, 245-248. | |||||
REF 42 | Inhibitory effect of inaperisone hydrochloride (inaperisone), a new centrally acting muscle relaxant, on the micturition reflex. Eur J Pharmacol. 1992 Mar 31;213(3):409-15. | |||||
REF 43 | 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 44 | 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. | |||||
REF 45 | 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 46 | The potential of subtype-selective neuronal nicotinic acetylcholine receptor agonists as therapeutic agents. Life Sci. 1998;62(17-18):1601-6. | |||||
REF 47 | Modulators of nicotinic acetylcholine receptors as analgesics. Curr Opin Investig Drugs. 2004 Jan;5(1):76-81. | |||||
REF 48 | Patent US20030087306 A1. | |||||
REF 49 | Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. | |||||
REF 50 | 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 51 | Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ. 1994 Oct;5(10):1033-40. | |||||
REF 52 | Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities. J Nat Prod. 2008 Jan;71(1):112-6. |
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