Altinicline
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Altinicline
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| Systematic (IUPAC) name | |
| (2S)-3-ethynyl-5-(1-methylpyrrolidin-2-yl)pyridine | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 179120-92-4 |
| ATC code | None |
| PubChem | CID 3036156 |
| ChemSpider | 2300234  |
| UNII | RJ9V9V09VM |
| ChEMBL | CHEMBL111659 |
| Chemical data | |
| Formula | C12H14N2 |
| Mol. mass | 186.252 |
| SMILES | eMolecules & PubChem |
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Altinicline (SIB-1508Y) 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] although its current status is unclear.
Chemistry
Wagner, Florence F.; Comins, Daniel L. (2006). "Expedient Five-Step Synthesis of SIB-1508Y from Natural Nicotine". The Journal of Organic Chemistry 71 (22): 8673. doi:10.1021/jo0616052. PMID 17064057.
References
- ^ Cosford, N. D.; Bleicher, L.; Vernier, J. M.; Chavez-Noriega, L.; Rao, T. S.; Siegel, R. S.; Suto, C.; Washburn, M. et al (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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