Phenylglycine derivatives as antagonists of metabotropic glutamate receptors

Metabotropic glutamate receptors represent a family of G protein-coupled receptors that can be activated by L-glutamate, the principal excitatory neurotransmitter in the brain. Until recently, progress in identifying the physiological and pathological roles of metabotropic glutamate receptors has been hampered by the lack of selective antagonists. In this article, Jeff Watkins and Graham Collingridge describe the pharmacology of, and initial physiological studies using, certain phenylglycine derivatives and related substances--the first definitive antagonists of metabotropic glutamate receptors.