Positive allosteric modulator of mGlu group I receptors (pEC50
value is 7.16 for the rat mGlu1a
receptor). Exhibits activity at all group I receptors, including human and rat mGlu1
and rat mGlu5
. Enhances the effects of (S
)-DHPG in CA3 neurons (EC50
= 95 nM).
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A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators.
Hemstapat et al.
Positive allosteric modulators of metabotropic glutamate receptor: Characterizationn, mechanism of action, and binding site.
Knoflach et al.