A-794278

Non Antibodies

mGluR1, mGluR5

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

342, 46

An Antagonist of mGluR1 and mGluR5

Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

A-794278 is a potent and selective noncompetitive mGluR1 antagonist, acting on mGluR1 and mGluR5 with IC50 values of 4.1 nM and 147 nM, respectively1. In vivo it shows analgesic properties, significantly attenuating spontaneous post-operative pain behavior in rats (ED50 = 50 μMol/kg)2.

Yes

A-794278 is a potent, non-competitive antagonist of mGluR1. It is a triazafluorenone derivative that also antagonizes mGluR5 receptors. It demonstrates IC50 values of 4.1 nM and 147 nM for mGluR1 and mGluR5, respectively1. A-794278 binds to a putative allosteric recognition site located within the seven-transmembrane domain of the receptor1, 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). mGluRs consist of three groups: I, II, and III 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 functions with potential implications in neurological and psychiatric disorders1, 2.