Chemistry:SIB-1757

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Short description: Chemical compound
SIB-1757
SIB-1757.svg
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC12H11N3O
Molar mass213.240 g·mol−1
3D model (JSmol)
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SIB-1757 is a drug used in scientific research which was one of the first compounds developed that acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR5.[1] It has anti-hyperalgesia effects in animals.[2] SIB-1757 along with other mGluR5 antagonists has been shown to have neuroprotective and hepatoprotective effects,[3][4] and it is also used to study the role of the mGluR5 receptor in brain development.[5]

References

  1. "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. July 1999. PMID 10381773. 
  2. "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. October 2000. doi:10.1016/S0304-3940(00)01458-0. PMID 10998562. 
  3. "Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice". Journal of Hepatology 38 (2): 179–87. February 2003. doi:10.1016/S0168-8278(02)00384-7. PMID 12547406. 
  4. "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. September 2003. doi:10.1046/j.1471-4159.2003.01932.x. PMID 12950444. 
  5. "Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons". Neuropharmacology. 49 Suppl 1: 104–13. 2005. doi:10.1016/j.neuropharm.2005.05.012. PMID 16005029.