- Lavreysen, H. et al. (2003) Mol. Pharmacol. 63, 1082.
- Alomone Labs R214127 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.Dose response of R214127 (#R-215) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization.
Cells were loaded with calcium-sensitive dye, incubated with a range of R214127 concentrations, and stimulated with 5 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
R214127 is a potent and selective non-competitive antagonist of mGluR1 displaying an IC50 value of 21.6 ± 5.0 nM1. The compound has minimal and nonspecific binding towards other mGlu receptors1.
Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs), members of G-protein coupled receptors (GPCRs). These receptors are divided into three groups based on sequence homology with a total of eight subtypes, mGluR1 to mGluR8.
mGluR1 plays an important role in the central sensitization of pain and in a variety of physiological functions including regulating ion channels, synaptic transmission and in synaptic plasticity that underlies learning and memory1,2.
R214127 (#R-215) is a highly pure, synthetic, and biologically active compound.