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Molecules 2011, 16(3), 2097-2106; doi:10.3390/molecules16032097
Review

Positive Allosteric Modulators of Type 5 Metabotropic Glutamate Receptors (mGluR5) and Their Therapeutic Potential for the Treatment of CNS Disorders

 and *
Received: 6 January 2011; in revised form: 8 February 2011 / Accepted: 28 February 2011 / Published: 2 March 2011
(This article belongs to the Special Issue Neuroactive Compounds)
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Abstract: Studies utilizing selective pharmacological antagonists or targeted gene deletion have demonstrated thattype 5 metabotropic glutamate receptors (mGluR5) are critical mediators and potential therapeutic targets for the treatment of numerous disorders of the central nervous system (CNS), including depression, anxiety, drug addiction, chronic pain, Fragile X syndrome, Parkinson’s disease, and gastroesophageal reflux disease. However, in recent years, the development of positive allosteric modulators (PAMs) of the mGluR5 receptor have revealed that allosteric activation of this receptor may also be of potential therapeutic benefit for the treatment of other CNS disorders, including schizophrenia, cognitive deficits associated with chronic drug use, and deficits in extinction learning. Here we summarize the discovery and characterization of various mGluR5 PAMs, with an emphasis on those that are systemically active. We will also review animal studies showing that these molecules have potential efficacy as novel antipsychotic agents. Finally, we will summarize findings that suggest that mGluR5 PAMs have pro-cognitive effects such as the ability toenhance synaptic plasticity, improve performance in various learning and memory tasks, including extinction of drug-seeking behavior, and reverse cognitive deficits produced by chronic drug use.
Keywords: glutamate; receptor; metabotropic; positive allosteric modulator; schizophrenia; addiction; learning; memory; synaptic plasticity glutamate; receptor; metabotropic; positive allosteric modulator; schizophrenia; addiction; learning; memory; synaptic plasticity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Cleva, R.M.; Olive, M.F. Positive Allosteric Modulators of Type 5 Metabotropic Glutamate Receptors (mGluR5) and Their Therapeutic Potential for the Treatment of CNS Disorders. Molecules 2011, 16, 2097-2106.

AMA Style

Cleva RM, Olive MF. Positive Allosteric Modulators of Type 5 Metabotropic Glutamate Receptors (mGluR5) and Their Therapeutic Potential for the Treatment of CNS Disorders. Molecules. 2011; 16(3):2097-2106.

Chicago/Turabian Style

Cleva, Richard M.; Olive, M. Foster. 2011. "Positive Allosteric Modulators of Type 5 Metabotropic Glutamate Receptors (mGluR5) and Their Therapeutic Potential for the Treatment of CNS Disorders." Molecules 16, no. 3: 2097-2106.


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