Fig. 2.

mGlu5 PAMs potentiate Glu-mediated pERK1/2 and show robust agonist activity. (A) In HEK293A cells expressing low levels of mGlu₅, 1 mM glutamate, 3 µM DPFE or 3 µM VU0364289 transiently increase levels of phosphorylated ERK1/2, peaking at 7 to 8 minutes and returning to baseline by 15 minutes, while vehicle has no effect. (B) Concentration response-curves reveal that DPFE and VU0364289 are more efficacious agonists than glutamate. (C) Increasing concentrations of DPFE raise baseline levels of pERK1/2 and shift the glutamate concentration-response curve to the left. Data represent the mean ± S.E.M. of three to six independent experiments performed in triplicate. Error bars not shown lie within the dimensions of the symbol.