VU6024578

VU6024578 (also known as BI02982816) is a small molecule positive allosteric modulator (PAM) of the metabotropic glutamate receptor 1 (mGlu1). It was developed through a collaboration between the Warren Center for Neuroscience Drug Discovery (WCNDD) at Vanderbilt University and Boehringer Ingelheim as a potential treatment for schizophrenia, specifically targeting both positive symptoms like psychosis and negative symptoms such as cognitive deficits. While the compound demonstrated efficacy in rodent models of hyperlocomotion and novel object recognition, its clinical development was halted due to species-specific adverse events observed in dogs, including salivation and rigidity. Despite this, VU6024578 remains a valuable rodent-selective tool compound for investigating the pharmacological role of mGlu1 in the central nervous system.