Metabotropic glutamate receptors (mGluRs) modulate brain excitability through diverse mechanisms. VU0361737 is a selective positive allosteric modulator (PAM) of mGluR4, displaying EC50 values of 110 and 240 nM for rat and human receptors, respectively. It has weak or no activity at other mGluRs. VU0361737 passes the blood-brain barrier to act centrally in rats. VU0361737, alone or in combination with an mGluR2 selective PAM, does not potentiate glutamate responses through mGlu2/4 heterodimers.
