SIB-1757

SIB-1757
IUPAC ime
6-metil-2-(fenilazo)-3-piridinol
Identifikatori
CAS broj31993-01-8 ДаY
ATC kodnone
PubChemCID 6849066
Hemijski podaci
FormulaC12H11N3O
Molarna masa213,235 g/mol
  • Oc1ccc(C)nc1\N=N\c2ccccc2

SIB-1757 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.[1] On ima antihipergleziono dejstvo kod životinja.[2] SIB-1757 zajedno sa drugim mGluR5 antagonistima ima neuroprotektivne i hepatoprotektivne efekte,[3][4] i on se takođe koristi u studiranju uloge mGluR5 receptora tokom moždanog razvoja.[5]

Reference

  1. ^ 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 (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. 
  2. ^ Dogrul A, Ossipov MH, Lai J, Malan TP, Porreca F (2000). „Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats”. Neuroscience Letters. 292 (2): 115—8. PMID 10998562. doi:10.1016/S0304-3940(00)01458-0. 
  3. ^ Storto M, Ngomba RT, Battaglia G, Freitas I, Griffini P, Richelmi P, Nicoletti F, Vairetti M (2003). „Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice”. Journal of Hepatology. 38 (2): 179—87. PMID 12547406. doi:10.1016/S0168-8278(02)00384-7. 
  4. ^ Fazal A, Parker F, Palmer AM, Croucher MJ (2003). „Characterisation of the actions of group I metabotropic glutamate receptor subtype selective ligands on excitatory amino acid release and sodium-dependent re-uptake in rat cerebrocortical minislices”. Journal of Neurochemistry. 86 (6): 1346—58. PMID 12950444. doi:10.1046/j.1471-4159.2003.01932.x. 
  5. ^ Bonsi P, Cuomo D, De Persis C, Centonze D, Bernardi G, Calabresi P, Pisani A (2005). „Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons”. Neuropharmacology. 49. Suppl 1: 104—13. PMID 16005029. doi:10.1016/j.neuropharm.2005.05.012. 

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