mGlu3 receptor is part of group II mGluRs (class C G Protein-Coupled Receptors) and inhibits adenylate cyclase, leading to a decrease in the second messenger cAMP in cells upon activation. The receptor is expressed both in neuronal and glial cells where it helps modulating glutamate action.
mGlu3 receptor activation or potentiation represents an exciting new avenue for treating neurodegenerative disorders such as Alzheimer’s, Parkinson’s or Huntington’s diseases. In particular, it has been shown that such an approach induces a neuroprotective effect, most probably mediated through a combined reduction of glutamate levels as well as stimulation of growth factor expression and production.
mGlu3 PAMs identified by Addex from within its corporate library of small molecules are unique starting points ready to enter lead optimisation. These NCEs show strong mGlu3 PAM activity, while also demonstrating exquisite selectivity versus all other mGlu receptor subtypes.