Abstract
Metabotropic glutamate type 7 (mGlu(7)) receptor is a member of the group III family of mGlu receptors. It is widely distributed in the central nervous system (CNS) and is preferentially expressed on presynaptic nerve terminals where it is thought to play a critical role in modulating normal neuronal function and synaptic transmission, making it particularly relevant in neuropharmacology. The lack of small-molecule mGlu7 ligands with adequate potency, selectivity and drug-like properties has resulted in difficulties in the preclinical validation of mGlu7 modulation in disease models. In the last decade, allosteric modulators of mGlu(7) receptors have emerged as valuable tools with good potency, selectivity and physicochemical properties to study and unleash the therapeutic potential of mGlu(7) receptors. This review focusses on the medicinal chemistry of mGlu(7) receptor allosteric ligands discovered since 2008.