Metabotropic Glutamate Receptors

Abstract

Since the first suggestion of G‐protein coupled glutamate receptor(s) and the subsequent cloning of eight different subtypes within the past 2 decades, our understanding of the neurophysiologic role and importance of the metabotropic glutamate (mGlu) receptors has greatly advanced, in large part owing to discovery and advancement of potent and selective pharmacological agents. These include orthosteric (i.e. N‐terminal glutamate‐site) agonists and antagonists possessing remarkable selectivity for one of the three mGlu receptor groups: Group I (mGlu1 and mGlu5), Group II (mGlu2 and mGlu3), or Group III (mGlu4, mGlu6, mGlu7 and mGlu8). More recently, subtype selective allosteric modulators that bind to the seven transmembrane (7‐TM) domain (potentiators, non‐competitive antagonists, and/or inverse agonists) for one or more of the eight mGlu receptor subtypes have been described. This chapter will focus on a brief description and summary of key findings for a number of these neuropharmacologic agents.