SIB-1757

• CAT Number: I009352
• CAS Number: 31993-01-8
• Molecular Formula: C12H11N3O
• Molecular Weight: 213.24
• Purity: ≥95%
• Synonyms: 6-methyl-2-phenyldiazenylpyridin-3-ol
• InChI: InChI=1S/C12H11N3O/c1-9-7-8-11(16)12(13-9)15-14-10-5-3-2-4-6-10/h2-8,16H,1H3
• InChIKey: LOCPVWIREQIGNQ-UHFFFAOYSA-N
• SMILES: CC1=NC(=C(C=C1)O)N=NC2=CC=CC=C2

SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM[1].
SIB-1757 (2 μM) reduces the 3,5-DHPG-induced membrane depolarization of the recorded neuron in striatal cholinergic interneurons[4].
SIB-1757 (20 mg/kg, i.p.) reduces the Acetaminophen (HY-66005) induced increased expression and activity of liver iNOS in mice[2].
SIB-1757 (intraplantar injection of 100 μg, or s.c. injection of 20 mg/kg) reverses spinal nerve ligation-induced thermal hyperalgesia in rats[3].

Reference

[1]. Varney MA, et al. SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J Pharmacol Exp Ther. 1999 Jul;290(1):170-81.
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[2]. Storto M, et al. Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice. J Hepatol. 2003 Feb;38(2):179-87.
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[3]. Dogrul A, et al. Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats. Neurosci Lett. 2000 Oct 6;292(2):115-8.
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[4]. Bonsi P, et al. Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons. Neuropharmacology. 2005;49 Suppl 1:104-13.
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