Altiniklin
 | |
| IUPAC ime | |
|---|---|
(2S)-3-etinil-5-(1-metilpirolidin-2-il)piridin | |
| Identifikatori | |
| CAS broj | 179120-92-4  |
| ATC kod | None |
| PubChem | CID 3036156 |
| ChemSpider | 2300234 |
| UNII | RJ9V9V09VM |
| ChEMBL | CHEMBL111659 |
| Hemijski podaci | |
| Formula | C12H14N2 |
| Molarna masa | 186.252 |
| |
| |
Altiniklin (SIB-1508Y) je lek koji deluje kao agonist na neuronskim nikotinskim acetilholinskim receptorima. On je visoko selektivan za α4β2 receptor.[1][2] Ovaj ligand stimuliše oslobađanje dopamina i acetilholina u mozgu kod glodara i primata.[3] On je izučavan do Faze II kliničkih ispitivanja za Parkinsonovu bolest.[4]
Hemija
[уреди | уреди извор]Jedan od sintetičkih puteva je:[5]
Reference
[уреди | уреди извор]- ^ Cosford, N. D.; Bleicher, L.; Vernier, J. M.; Chavez-Noriega, L.; Rao, T. S.; Siegel, R. S.; Suto, C.; Washburn, M.; Lloyd, G. K. (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. PMID 10812948. doi:10.1016/S0031-6865(99)00024-2.
- ^ Wagner, F.; Comins, D. (2006). „Expedient five-step synthesis of SIB-1508Y from natural nicotine”. The Journal of Organic Chemistry. 71 (22): 8673—8675. PMID 17064057. doi:10.1021/jo0616052.
- ^ 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. PMID 18692487. doi:10.1016/j.brainres.2008.07.063.
- ^ The Parkinson Study Group (2006). „Randomized placebo-controlled study of the nicotinic agonist SIB-1508Y in Parkinson disease”. Neurology. 66: 408—410. doi:10.1212/01.wnl.0000196466.99381.5c.
- ^ 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. PMID 17064057. doi:10.1021/jo0616052.
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