SIB-1893 explained
SIB-1893 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 anticonvulsant and neuroprotective effects,[2] and reduces glutamate release.[3] It has also been found to act as a positive allosteric modulator of mGluR4.[4]
Notes and References
- 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 . 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 . 10381773 .
- Chapman AG, Nanan K, Williams M, Meldrum BS . 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 . July 2000 . 10854901 . 10.1016/S0028-3908(99)00242-7. 21528282 .
- Wang SJ, Sihra TS . 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 . June 2004 . 14982967 . 10.1124/jpet.103.064881 . 800526 .
- Mathiesen JM, Svendsen N, Bräuner-Osborne H, Thomsen C, Ramirez MT . Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP . . 138 . 6 . 1026–30 . March 2003 . 12684257 . 1573757 . 10.1038/sj.bjp.0705159 .