Metabotropic glutamate receptors (mGluRs) modulate brain excitability through diverse mechanisms.{21634} VU0361737 is a selective positive allosteric modulator (PAM) of mGluR4, displaying EC50 values of 110 and 240 nM for rat and human receptors, respectively.{27968} It has weak or no activity at other mGluRs.{27968} VU0361737 passes the blood-brain barrier to act centrally in rats.{27968,27969} VU0361737, alone or in combination with an mGluR2 selective PAM, does not potentiate glutamate responses through mGlu2/4 heterodimers.{27970}
产品描述
A selective PAM of mGluR4, displaying EC50 values of 110 and 240 nM for rat and human receptors, respectively; passes the blood-brain barrier to act centrally in rats
