Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders.  WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636.  The authors show that CVN636 has high selectivity toward mGluR7, with CNS penetrance and efficacy in an in vivo rodent model of alcohol use disorder.