Fig. 2.

DN10 and DN13 are positive allosteric modulators of mGlu2. a Cartoon illustrating the principle of the mGlu2 sensor assay, where the VFT movement associated with receptor activation results in a decrease in TR-FRET signal measured between Lumi4-Tb and SNAP-Green labeled SNAP tags. b DN10 and DN13 dose-dependently decrease the sensor signal in the presence of EC₂₀ concentration of agonist LY379268 (0.1 nM), indicative of receptor activation. DN10 c and DN13 d dose-dependently potentiate the effect of LY379268 on the mGlu2 sensor. DN10 e and DN13 f dose-dependently potentiate the effect of LY379268 on the production of inositol phosphate in mGlu2-transfected cells. EAAC1 was co-transfected with mGlu2 to decrease the ambient glutamate concentration. Note that the lower the IP-One Gq HTRF ratio, the higher the amount of inositol monophosphate produced (IP1). Data are mean ± SEM of three individual experiments each performed in triplicates