Ispronicline

Drugbox
IUPAC_name = (E,2S)-N-methyl-5-(5-propan-2-yloxypyridin-3-yl)pent-4-en-2-amine

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width= 240
CAS_number= 252870-53-4
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PubChem= 9824145
DrugBank=
C=14 | H=22 | N=2 | O=1
molecular_weight = 234.336
smiles = CC(C)Oc1cncc(C=CCC(C)NC)c1
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Ispronicline (TC-1734, AZD-3480) is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects, and is under development for the treatment of dementia and Alzheimer's disease. Clinical trials so far have shown ispronicline to be effective and well tolerated, with the main side effects being dizziness and headache. [Gatto GJ, Bohme GA, Caldwell WS, Letchworth SR, Traina VM, Obinu MC, Laville M, Reibaud M, Pradier L, Dunbar G, Bencherif M. TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects. "CNS Drug Reviews". 2004 Summer;10(2):147-66. PMID 15179444] [Dunbar G, Demazières A, Monreal A, Cisterni C, Metzger D, Kuchibhatla R, Luthringer R. Pharmacokinetics and safety profile of ispronicline (TC-1734), a new brain nicotinic receptor partial agonist, in young healthy male volunteers. "Journal of Clinical Pharmacology". 2006 Jul;46(7):715-26. PMID 16809797] [Lippiello P, Letchworth SR, Gatto GJ, Traina VM, Bencherif M. Ispronicline: a novel alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties. "Journal of Molecular Neuroscience". 2006;30(1-2):19-20. PMID 17192610] [Dunbar G, Boeijinga PH, Demazières A, Cisterni C, Kuchibhatla R, Wesnes K, Luthringer R. Effects of TC-1734 (AZD3480), a selective neuronal nicotinic receptor agonist, on cognitive performance and the EEG of young healthy male volunteers. "Psychopharmacology (Berlin)". 2007 May;191(4):919-29. PMID 17225162] [Dunbar GC, Inglis F, Kuchibhatla R, Sharma T, Tomlinson M, Wamsley J. Effect of ispronicline, a neuronal nicotinic acetylcholine receptor partial agonist, in subjects with age associated memory impairment (AAMI). "Journal of Psychopharmacology". 2007 Mar;21(2):171-8. PMID 17329297]

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