VU0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax. Its site of action is distinct from the classical mGlu5 negative allosteric modulator (NAM) MPEP allosteric site or the site of a recetly discovered PAM, CPPHA. However, VU0357121shares a functional interaction with the MPEP site. VU0357121 is highly selective for activation of mGlu5 and is inactive or very weakly antagonizing at other mGlu receptor subtypes.
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