Chemistry:Altinicline

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Short description: Chemical compound
Altinicline
Altinicline.svg
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC12H14N2
Molar mass186.252 g·mol−1
3D model (JSmol)
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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

  1. "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): 125–30. March 2000. doi:10.1016/S0031-6865(99)00024-2. PMID 10812948. 
  2. "Expedient five-step synthesis of SIB-1508Y from natural nicotine". The Journal of Organic Chemistry 71 (22): 8673–5. October 2006. doi:10.1021/jo0616052. PMID 17064057. 
  3. "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. October 2008. doi:10.1016/j.brainres.2008.07.063. PMID 18692487. 
  4. The Parkinson Study Group (February 2006). "Randomized placebo-controlled study of the nicotinic agonist SIB-1508Y in Parkinson disease". Neurology 66 (3): 408–10. doi:10.1212/01.wnl.0000196466.99381.5c. PMID 16476941.