Altinicline (SIB-1508Y , SIB-1765F ) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype.[1] [2] It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models,[3] and progressed as far as Phase II clinical trials for Parkinson's disease ,[4] where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear.
References [ edit ]
^ Cosford, N. D.; Bleicher, L.; Vernier, J. M.; Chavez-Noriega, L.; Rao, T. S.; Siegel, R. S.; Suto, C.; Washburn, M.; Lloyd, G. K.; McDonald, I. A. (2000). "Recombinant human receptors and functional assays in the discovery of altinicline (SIB-1508Y), a novel acetylcholine-gated ion channel (nAChR) agonist". Pharmaceutica acta Helvetiae . 74 (2–3): 125–130. doi :10.1016/S0031-6865(99)00024-2 . PMID 10812948 .
^ Wagner, F.; Comins, D. (2006). "Expedient five-step synthesis of SIB-1508Y from natural nicotine". The Journal of Organic Chemistry . 71 (22): 8673–8675. doi :10.1021/jo0616052 . PMID 17064057 .
^ Rao, T.; Adams, P.; Correa, L.; Santori, E.; Sacaan, A.; Reid, R.; Cosford, N. (2008). "Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist". Brain Research . 1234 : 16–24. doi :10.1016/j.brainres.2008.07.063 . PMID 18692487 .
^ The Parkinson Study Group. Randomized placebo-controlled study of the nicotinic agonist SIB-1508Y in Parkinson disease. Neurology . 2006;66:408-410. doi :10.1212/01.wnl.0000196466.99381.5c
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