Figure 2.

Quantitation of single cell Ca²⁺ imaging showing cell-type and location-dependent bias of tested mGlu₅ NAMs. Compiled data from Quis-induced Ca²⁺ responses (10 μM) as normalized fluorescence response (% Quis) following pretreatment with MPEP, Fenobam, RG7090, AZD2066, or AFQ056, at the indicated concentrations in mGlu₅/HEK cells and hippocampal and striatal neurons. At 5 and 10 μM, all NAMs tested blocked Quis-induced Ca²⁺ responses in HEK cells or hippocampal neurons whereas AFQ056 did not completely block the Quis-induced Ca²⁺ rise in striatal neurons at any dose. At 1 μM, Fenobam was less effective in mGlu₅/HEK, hippocampal and striatal cells as well. Bars represent the mean of three independent experiments ± SEM from 80 to 100 neurons/condition. **Denotes statistical significance compared with control (Quis only) with Student’s t test (**p < 0.01, ***p < 0.001).