| 词条 | Ispronicline |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 444274830 | IUPAC_name = (2S,4E)-5-(5-isopropoxypyridin-3-yl)-N-methylpent-4-en-2-amine | image = Ispronicline.png | width = 240 | tradename = | routes_of_administration = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 252870-53-4 | ATC_prefix = none | ATC_suffix = | PubChem = 9824145 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3E05NBH9V5 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08935 | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 7999892 | C=14 | H=22 | N=2 | O=1 | molecular_weight = 234.336 | smiles = C[C@@H](C/C=C/C1=CC(=CN=C1)OC(C)C)NC | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C14H22N2O/c1-11(2)17-14-8-13(9-16-10-14)7-5-6-12(3)15-4/h5,7-12,15H,6H2,1-4H3/b7-5+/t12-/m0/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = RPCVIAXDAUMJJP-PZBABLGHSA-N }}Ispronicline (TC-1734, AZD-3480) is an experimental drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease, but is no longer under development.[1] Ispronicline is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects.{{medcn|date=July 2014}} Early stage clinical trials showed that ispronicline was well tolerated, with the main side effects being dizziness and headache.[2][3][4][5][6] However, mid stage clinical trials failed to show sufficient efficacy to continue development as a pharmaceutical drug.[1] References1. ^1 Targacept Drops Development of Alzheimer's Drug {{Stimulants}}{{Nootropics}}{{Antidementia}}{{Antidepressants}}{{Nicotinic acetylcholine receptor modulators}}{{nervous-system-drug-stub}}2. ^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}} 3. ^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}} 4. ^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}} 5. ^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. 2007 May;191(4):919-29. {{DOI|10.1007/s00213-006-0675-x}} {{PMID|17225162}} 6. ^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}} 8 : Nootropics|Pyridines|Nicotinic agonists|Stimulants|Ethers|Amines|Isopropyl compounds|Alkenes |
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