Figure 3. Potency and efficacy of the novel mGluR4 PAM, CID 44191096.

Figure 3Potency and efficacy of the novel mGluR4 PAM, CID 44191096

(a) CID 44191096 was added in progressively higher concentrations to cell co-expressing human mGluR4 and the chimeric G protein Gqi5 (white boxes). After a 2.5 minute incubation period, an EC20 concentration of glutamate was added (black boxes) and the change in fluorescence was monitored using a kinetic imaging plate reader. Data are three independent determinations performed in triplicate. (b) Either DMSO vehicle or a 30 μM concentration of CID 44191096 was incubated with human mGluR4/Gqi5 cells and 2.5 minutes later increasing concentrations of glutamate were added. In this experiment, performed in triplicate and representative of three independent determinations, CID 44191096 shifted the glutamate concentration-response curve 33 fold to the left

From: Discovery of a potent, selective and in vivo active mGluR4 positive allosteric modulator

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