TTD Target ID: TTDS00303

Target Information
Name	Nicotinic acetylcholine receptor
Type of target	Successful target
Synonyms	Nicotinergic acetylcholine receptor
	nAChR
Disease	Alcoholism    [1]
	Alzheimer's disease    [2][3]
	Analgesics    [4]
	Cancer, unspecific    [5]
	Cognitive deficits    [6]
	Depression    [7]
	Drug dependence    [8]
	Gilles de la Tourette's disorder    [9]
	Helminth infection    [10]
	Mood [affective] disorders    [11]
	Neuropsychiatric disorders    [8]
	Pain    [4]
	Parkinson's disease    [8][12][9]
Drug(s)	Atracurium		Approved	General anesthesia	[13][14][15]
	Benztropine mesylate		Approved	Parkinson's Disease	[16]
	Cisatracurium Besylate		Approved	General anesthesia	[13][17]
	Mecamylamine		Approved	Hypertension	[18]
	Nicotine		Approved	Nicotine dependence	[19][20]
	Pancuronium		Approved	Anesthetic	[13]
	Varenicline tartrate		Launched	Tobacco dependence	[21]
	TRIDMAC		Phase II	Severe Mood Disorders	[22]
	ABT-089		Discontined in Phase II	Attention-defi cit/hyperactivity disorder, schizophrenia, anxiety and dementia	[23]
	AZD0328		Terminated in Phase II	Alzheimer's disease; Schizophrenia	[24][25]
	Dexefaroxan		Discontinued in Phase II	Schizophrenia	[26]
	Dianicline		Discontinued in Phase III	Tobacco dependence	[21]
	Dianicline+rimonabant		Discontinued	Tobacco dependence	[21]
	NAChRs agonist		Preclinical	Parkinson¡¯s Disease	[16]
BioChemical Class	Ion transport
Related US Patent	6,277,855
	6,448,276
Target Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	PROTOSTEMODIOL		[27]
Agonist	A-85380		[28]
	ABT-089		[23]
	ABT-418		[6]
	ABT-594		[29][30]
	AZD0328		[24][25]
	DBO-83		[28]
	Dexefaroxan		[26]
	Dianicline		[21]
	Dianicline+rimonabant		[21]
	Epibatidine		[31]
	NAChRs agonist		[16]
	RJR-2403		[28]
	SIB-1508Y		[7][12]
	SIB-1553A		[31]
	SIB-1663		[28]
	SIB-1765F		[32]
	Varenicline tartrate		[21]
Antagonist	Atracurium		[13][14][15]
	Benztropine mesylate		[16]
	Cisatracurium Besylate		[13][17]
	Hexamethonium		[5]
	Mecamylamine		[18]
	Nicotine		[19][20]
	Pancuronium		[13]
	TRIDMAC		[22]
Multitarget	Dexefaroxan		[26]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Accumbal 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 2	Cholinergic regulation of synaptic plasticity as a therapeutic target in Alzheimer's disease. J Alzheimers Dis. 2002 Oct;4(5):349-55. To Reference
Ref 3	Nicotine 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 4	Antagonist 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 5	Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ. 1994 Oct;5(10):1033-40. To Reference
Ref 6	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. To Reference
Ref 7	Antidepressant-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 8	Subunit 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 9	Novel 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 10	Cyclooctadepsipeptides--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 11	Nicotinic acetylcholine receptors as targets for antidepressants. Mol Psychiatry. 2002;7(6):525-35. To Reference
Ref 12	Nicotinic 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 13	Pharmacological 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 14	Neuromuscular block. Br J Pharmacol. 2006 Jan;147 Suppl 1:S277-86. To Reference
Ref 15	Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51. To Reference
Ref 16	Drugs 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 17	Comparative 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 18	Mecamylamine (Inversine): an old antihypertensive with new research directions. J Hum Hypertens. 2002 Jul;16(7):453-7. To Reference
Ref 19	Atypical 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 20	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. To Reference
Ref 21	Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. To Reference
Ref 22	Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 23	Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34. To Reference
Ref 24	AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 25	AstraZeneca. Report of AstraZeneca. 31 January 2008. To Reference
Ref 26	The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 27	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. To Reference
Ref 28	The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control. Expert Opin Investig Drugs. 2001 Oct;10(10):1819-30. To Reference
Ref 29	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. To Reference
Ref 30	The 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 31	The potential of subtype-selective neuronal nicotinic acetylcholine receptor agonists as therapeutic agents. Life Sci. 1998;62(17-18):1601-6. To Reference
Ref 32	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. To Reference

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Professor in Department of Pharmacy
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