Overview
Alomone Labs DM-PPP inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.Dose response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by DM-PPP (#D-255). IC50 was determined at 144 nM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with different concentrations of DM-PPP, and stimulated by 15 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
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- Eom, H.S. et al. (2016) PLoS One 11, e0147538.
DM-PPP is a synthetic compound that acts as a selective and non-competitive antagonist of mGluR1 receptors with an IC50 value of 15.8 nM1. The compound interacts with the 7 transmembrane (7TM) domain of the receptor. In several animal models DM-PPP shows antinociceptive properties1.
Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly expressed on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus2.
DM-PPP (#D-255) is a highly pure, synthetic, and biologically active compound.
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