Overview
- Schoepp, D.D. et al. (1999) Neuropharmacology 38, 1431.
Centrifuge all product preparations before use (10000 x g 5 min).
Alomone Labs DL-AP3 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.Dose-response of DL-AP3 (#D-275) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of DL-AP3 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™. IC50 was determined at 295 µM.
DL-AP3 is a racemic compound of 2-amino-3-phosphonopropionic acid that acts as a potent and competitive antagonist of mGluR1 receptors. It demonstrates an IC50 value of 1 mM for rat mGluR1 when challenged with glutamate2. DL-AP3 has neuroprotective effects in the gerbil model of global ischemia1,2.
Glutamate is the most abundant excitatory neurotransmitter in the central nervous system. It modulates the activity of many types of synapses by activating, in part, 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. Type 1 mGluRs are mainly detected on post-synaptic neurons and affect the fate of neuronal progenitor cells and neural stem cells, and are important for the formation of the hippocampus3.
