Overview
- Litschig, S. et al. (1999) Mol. Pharmacol. 55, 453.
- Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
Alomone Labs CPCCOEt inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.Dose-response of CPCCOEt (#C-370) normalized inhibition of human mGluR1-mediated, L-glutamate-evoked Ca2+ mobilization. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with varying CPCCOEt concentrations, and stimulated by 5 µM L-glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
CPCCOEt is a compound that acts as a selective, non-competitive antagonist of mGluR1. It can inhibit mGluR1 signaling without affecting glutamate binding1. CPCCOEt selectively inhibits mGluR1b-induced increases in intracellular calcium and demonstrates IC50 of 6.5 µM1.
Glutamate is the most abundant excitatory neurotransmitter in the central nervous system. It modulates the activity of many types of synapses by activating metabotropic glutamate receptors (mGluRs), members of the G-protein coupled receptor (GPCR) superfamily. These receptors are divided into three groups based on sequence homology with a total of eight subtypes, mGluR1 to mGluR8.
mGluR1 from group I, plays an important role in the central sensitization of pain and in a variety of physiological functions including regulation of ion channels, synaptic transmission, and plasticity1,2.
