Figure 1.

Modulator potency curves for enhancement of glutamate stimulation of mGlu₅ iCa²⁺mobilization. (a) Structures of a validation set of 10 mGlu₅ PAMs. (b, c) Modulation of glutamate stimulation of iCa²⁺ mobilization in HEK cells expressing the rat mGlu_5a. Increasing concentrations of indicated modulator were added prior to a concentration of glutamate that elicits a 20% maximal response (b, c). The glutamate control curve is shown in gray squares. Data were normalized to the maximal glutamate (1 mM) response and fit with a 4-parameter logistic equation. Data are mean ± s.e.m. of three independent determinations performed in triplicate.