Therapeutic Targets Database
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TTD Target ID: TTDS00303

Target Information
NameNicotinic acetylcholine receptor    
Type of targetSuccessful target    
SynonymsNicotinergic acetylcholine receptor    
nAChR    
DiseaseAlcoholism
[ICD9: 303   ICD10: F10.2]
[1]
Alzheimer's disease
[ICD9: 331.0   ICD10: G30]
[2][3]
Analgesics
[ICD9: 338   ICD10: R52]
[4]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[5]
Cognitive deficits
[ICD9: 290-294, 294.0, 780.09, 780.9, 780.93   ICD10: F01-F07, F04, R41.3]
[6]
Depression
[ICD9: 311   ICD10: F32]
[7]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
[8]
Gilles de la Tourette's disorder[9]
Helminth infection
[ICD9: 001-139   ICD10: A00-B99]
[10]
Mood [affective] disorders[11]
Neuropsychiatric disorders[8]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[4]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[8][12][9]
Drug(s)AtracuriumApprovedGeneral anesthesia[13][14][15]
Benztropine mesylateApprovedParkinson's Disease[16]
Cisatracurium BesylateApprovedGeneral anesthesia[13][17]
CotinineApprovedInsecticide[18][19][20]
MecamylamineApprovedHypertension[21]
NicotineApprovedNicotine dependence [22][23]
PancuroniumApprovedAnesthetic[13]
Varenicline tartrateLaunchedTobacco dependence[24]
TRIDMACPhase IISevere Mood Disorders[25]
ABT-089Discontined in Phase IIAttention-defi cit/hyperactivity disorder, schizophrenia, anxiety and dementia[26]
AZD0328Terminated in Phase IIAlzheimer's disease; Schizophrenia[27][28]
DexefaroxanDiscontinued in Phase IISchizophrenia[29]
DianiclineDiscontinued in Phase IIITobacco dependence[24]
Dianicline+rimonabantDiscontinuedTobacco dependence[24]
NAChRs agonistPreclinicalParkinsoní»s Disease[16]
BioChemical ClassIon transport    
Related US Patent6,277,855
6,448,276
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorPROTOSTEMODIOL[30]
AgonistA-85380[31]
ABT-089[26]
ABT-418[6]
ABT-594[32][33]
AZD0328[27][28]
DBO-83[31]
Dexefaroxan[29]
Dianicline[24]
Dianicline+rimonabant[24]
Epibatidine[34]
NAChRs agonist[16]
RJR-2403[31]
SIB-1508Y[7][12]
SIB-1553A[34]
SIB-1663[31]
SIB-1765F[35]
Varenicline tartrate[24]
AntagonistAtracurium[13][14][15]
Benztropine mesylate[16]
Cisatracurium Besylate[13][17]
Hexamethonium[5]
Mecamylamine[21]
Nicotine[22][23]
Pancuronium[13]
TRIDMAC[25]
MultitargetDexefaroxan[29]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Accumbal dopamine overflow after ethanol: localization of the antagonizing effect of mecamylamine. Eur J Pharmacol. 1997 Sep 10;334(2-3):149-56. To Reference
Ref 2Cholinergic regulation of synaptic plasticity as a therapeutic target in Alzheimer's disease. J Alzheimers Dis. 2002 Oct;4(5):349-55. To Reference
Ref 3Nicotine increases the expression of high affinity nerve growth factor receptors in both in vitro and in vivo. Life Sci. 2002 Feb 15;70(13):1543-54. To Reference
Ref 4Antagonist of nicotinic acetylcholine receptors (nAChR) enhances formalin-induced nociception in rats: tonic role of nAChRs in the control of pain following injury. Brain Res. 2001 Jan 5;888(1):102-106. To Reference
Ref 5Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ. 1994 Oct;5(10):1033-40. To Reference
Ref 6Enhancement 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. To Reference
Ref 7Antidepressant-like effects of the subtype-selective nicotinic acetylcholine receptor agonist, SIB-1508Y, in the learned helplessness rat model of depression. Psychopharmacology (Berl). 2000 Oct;152(3):295-303. To Reference
Ref 8Subunit composition of functional nicotinic receptors in dopaminergic neurons investigated with knock-out mice. J Neurosci. 2003 Aug 27;23(21):7820-9. To Reference
Ref 9Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis. J Med Chem. 2000 Jun 1;43(11):2217-26. To Reference
Ref 10Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Int J Antimicrob Agents. 2003 Sep;22(3):318-31. To Reference
Ref 11Nicotinic acetylcholine receptors as targets for antidepressants. Mol Psychiatry. 2002;7(6):525-35. To Reference
Ref 12Nicotinic acetylcholine receptor agonist SIB-1508Y improves cognitive functioning in chronic low-dose MPTP-treated monkeys. J Pharmacol Exp Ther. 1999 Aug;290(2):731-9. To Reference
Ref 13Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. To Reference
Ref 14Neuromuscular block. Br J Pharmacol. 2006 Jan;147 Suppl 1:S277-86. To Reference
Ref 15Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. To Reference
Ref 16Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. To Reference
Ref 17Comparative study of neuromuscular blocking and hemodynamic effects of rocuronium and cisatracurium under sevoflurane or total intravenous anesthesia. Middle East J Anesthesiol. 2009 Feb;20(1):39-51. To Reference
Ref 1812008000 To Reference
Ref 19Plant Based Drugs and Medicines, by Leslie Taylor, in Raintree Nutrition, Inc., on October 13, 2000 To Reference
Ref 20Needs for new plant-derived pharmaceuticals in the post-genome era an industrial view in drug research and development, 2008 by Ying Wang To Reference
Ref 21Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7. To Reference
Ref 22Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors. Neuropharmacology. 2009 Aug;57(2):183-91. Epub 2009 May 28. To Reference
Ref 23Development 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. To Reference
Ref 24Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. To Reference
Ref 25Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 26Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. To Reference
Ref 27AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 28AstraZeneca. Report of AstraZeneca. 31 January 2008. To Reference
Ref 29The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 30J Nat Prod. 2008 Jan;71(1):112-6. Epub 2007 Dec 29.Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities. To Reference
Ref 31The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin Investig Drugs. 2001 Oct;10(10):1819-30. To Reference
Ref 32ABT-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. To Reference
Ref 33The nicotinic acetylcholine receptor agonist ABT-594 increases FGF-2 expression in various rat brain regions. Neuroreport. 1999 Dec 16;10(18):3909-13. To Reference
Ref 34The potential of subtype-selective neuronal nicotinic acetylcholine receptor agonists as therapeutic agents. Life Sci. 1998;62(17-18):1601-6. To Reference
Ref 35Interactions 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. To Reference



 

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