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 cells^1,2. 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.