SIB 1893 is a highly selective non-competitive antagonist for the mGluR-5 (metabotropic glutamate receptor 5 type); displays an IC50 value of 0.3 μM at hmGluR-5, compared with > 100 μM at hmGluR-1b, hmGluR-2, hmGluR-6, hmGluR-7 and hmGluR-8.
Varney et al (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J.Pharmacol.Exp.Ther. 290 170. Chapman et al (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 1567. Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026.
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