Altiniklin

Из Википедије, слободне енциклопедије
Altiniklin
(IUPAC) ime
(2S)-3-etinil-5-(1-metilpirolidin-2-il)piridin
Klinički podaci
Identifikatori
CAS broj 179120-92-4
ATC kod nije dodeljen
PubChem[1][2] 3036156
ChemSpider[3] 2300234
UNII RJ9V9V09VM YesY
ChEMBL[4] CHEMBL111659 YesY
Hemijski podaci
Formula C12H14N2 
Mol. masa 186.252
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Altiniklin (SIB-1508Y) je lek koji deluje kao agonist na neuronskim nikotinskim acetilholinskim receptorima. On je visoko selektivan za α4β2 receptor.[5][6] Ovaj ligand stimuliše oslobađanje dopamina i acetilholina u mozgu kod glodara i primata.[7] On je izučavan do Faze II kliničkih ispitivanja za Parkinsonovu bolest.[8]

Hemija[уреди]

Jedan od sintetičkih puteva je:[9]

Altinicline synth.png

Reference[уреди]

  1. ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.“. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ^ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities“. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ^ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining“. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ^ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery“. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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
  9. ^ 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.