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 memory^1,2.