Overview
- Fukuda, J. et al. (2009) Neuropharmacology 57, 438.
Alomone Labs LY456066 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.Dose-response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by LY456066 (#L-240). IC50 was determined at 14.9 nM. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of LY456066, 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™.
LY456066 is a selective, negative allosteric modulator of mGluR1 receptors. The compound demonstrates high potent antagonistic activities toward both rat and human mGluR1 receptor with an IC50 value of 28 nM for human mGluR1 receptors expressed in Chinese hamster ovary cells1,2. Several studies have suggested that LY456066 may bind to a site at the mGluR1 receptor that could represent a conserved negative allosteric regulatory domain3.
Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neurophysiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus4.
