Spooren WPJM; Gasparini F; Salt TE; Kuhn R; (2001) Novel allosteric antagonists shed light on mGluR5 receptors and CNS disorders. Trends in Pharmacological Sciences, 22: 331-337.

Although multiple metabotropic glutamate (mglu) receptor subtypes were cloned in the early 1990s, progress in the characterization of these receptors has been slow because of difficulties in obtaining subtype-selective ligands. However, in the past few years exciting progress has been made on the mglu5 receptor subtype following the identification of selective non-amino-acid-like ligands that implicate the mglu5 receptor as a potentially important therapeutic target, particularly for the treatment of pain and anxiety.

Author Keywords: mGluR5 antagonists; MPEP; non-competitive; CNS; animal models; pain; anxiety