RO4491533


RO-4491533 is a drug developed by Hoffmann-La Roche which acts as a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors, being equipotent at mGluR2 and mGluR3 but without activity at other mGluR subtypes. In animal studies, RO-4491533 produced antidepressant effects and reversed the effects of the mGluR2/3 agonist LY-379,268 with similar efficacy but slightly lower potency than the mGluR2/3 antagonist LY-341,495. A number of related compounds are known, with similar effects in vitro and a fairly well characterized structure-activity relationship.