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Abstract
Background: Glutamate mediates its effects via ionotropic and metabotropic glutamate (mGlu) receptors. mGlu receptors are G protein-coupled receptors that are classified into three clusters, group I-III. This review focuses on the mGlu5 receptors of group I. mGlu5 receptors are highly expressed in limbic brain regions and are located postsynaptically. Objective: Following the discovery of the prototypical negative allosteric modulator MPEP, the therapeutic potential of mGlu5 receptors has been steadily explored and expanded. This review highlights present developments in drug discovery and the therapeutic potential of negative allosteric modulators. Methods: Material evaluated ranged from patents to published literature, but also included information that is available from public-accessible websites. Results/conclusion: Based on the wide and consistent effects of prototypical antagonists, such as MPEP, it is concluded that mGlu5 receptor antagonists have treatment potential for both peripheral and central nervous system disorders ranging from psychiatric, neurological to neuromuscular, including illnesses with no apparent nervous system link, such as cancer.
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Acknowledgements
T Ballard, P Malherbe and E Vieira are gratefully acknowledged for valuable discussions and proof reading.