Overview
- Malherbe, P. et al. (2003) J. Biol. Chem. 278, 8340.
Alomone Labs EM-TBPC inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.Dose response of normalized inhibition of human mGluR1 receptors mediated, L-Glutamate evoked Ca2+ mobilization by EM-TBPC (#E-165). IC50 was determined at 370 nM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with a range of concentrations of EM-TBPC, 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™.
- Malherbe, P. et al. (2003) J. Biol. Chem. 278, 8340.
- Eom.HS. et al. (2016) PLoS One 11, e0147538.
EM-TBPC is a synthetic compound that acts as a potent, selective and noncompetitive antagonist of rat mGluR1 receptors with an IC50 value of 128 for rat mGluR1 expressed in HEK 293 cells. It displays very low affinity for human mGluR1 receptors. The binding pocket of EM-TBPC has been localized at the 7 transmembrane (7TM) domain of mGluR11.
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.
EM-TBPC (#E-165) is a highly pure, synthetic, and biologically active compound.
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