SIB-1893

Из Википедије, слободне енциклопедије
SIB-1893
(IUPAC) ime
(E)-2-metil-6-(2-feniletenil)piridin
Klinički podaci
Identifikatori
CAS broj 6266-99-5
ATC kod nije dodeljen
PubChem[1][2] 235382
ChEMBL[3] CHEMBL88612 YesY
Hemijski podaci
Formula C14H13N 
Mol. masa 195,259 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SIB-1893 je lek koji se koristi u naučnim istraživanjima. On je bio jedan od prvih jedinjenja razvijenih kao selektivni antagonisti za metabotropni glutamatni receptor podtip mGluR5.[4] On ima antikonvulsivno i neuroprotektivno dejstvo,[5] i redukuje otpuštanje glutamata.[6] On takođe deluje kao pozitivni alosterni modulator mGluR4 receptora.[7]

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. ^ 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
  4. ^ Varney MA, Cosford ND, Jachec C, Rao SP, Sacaan A, Lin FF, Bleicher L, Santori EM, Flor PJ, Allgeier H, Gasparini F, Kuhn R, Hess SD, Veliçelebi G, Johnson EC (July 1999). „SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5“. The Journal of Pharmacology and Experimental Therapeutics 290 (1): 170–81. PMID 10381773. 
  5. ^ Chapman AG, Nanan K, Williams M, Meldrum BS (July 2000). „Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893)“. Neuropharmacology 39 (9): 1567–74. DOI:10.1016/S0028-3908(99)00242-7. PMID 10854901. 
  6. ^ Wang SJ, Sihra TS (June 2004). „Noncompetitive metabotropic glutamate5 receptor antagonist (E)-2-methyl-6-styryl-pyridine (SIB1893) depresses glutamate release through inhibition of voltage-dependent Ca2+ entry in rat cerebrocortical nerve terminals (synaptosomes)“. The Journal of Pharmacology and Experimental Therapeutics 309 (3): 951–8. DOI:10.1124/jpet.103.064881. PMID 14982967. 
  7. ^ Mathiesen JM, Svendsen N, Bräuner-Osborne H, Thomsen C, Ramirez MT (March 2003). „Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP“. British Journal of Pharmacology 138 (6): 1026–30. DOI:10.1038/sj.bjp.0705159. PMC 1573757. PMID 12684257. 

Spoljašnje veze[уреди]