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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Unveiling the Functions of Presynaptic Metabotropic Glutamate Receptors in the Central Nervous System

Darryle D. Schoepp
Journal of Pharmacology and Experimental Therapeutics October 2001, 299 (1) 12-20;
Darryle D. Schoepp
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Abstract

Metabotropic glutamate (mGlu) receptors, which include mGlu1–8 receptors, are a heterogeneous family of G-protein-coupled receptors which function to modulate brain excitability via presynaptic, postsynaptic and glial mechanisms. Certain members of this receptor family have been shown to function as presynaptic regulatory mechanisms to control release of neurotransmitters. In general, Gi-coupled mGlu receptor subtypes appear to negatively modulate excitatory (and possibly also inhibitory) neurotransmitter output when activated. Localization studies have shown that mGlu7 is restricted to the presynaptic grid at the site of vesicle fusion. These studies along with other evidence suggest that mGlu7 is the nerve terminal autoreceptor that regulates physiological release of glutamate. Other mGlu subtypes, in particular mGlu2, mGlu8, and possibly mGlu4, are also localized presynaptically, but at perisynaptic sites outside the active zone of neurotransmitter release. Gi-coupled mGlu receptors also may exist on presynaptic elements of neighboring γ-aminobutyric acid (GABA) neurons where they play a role in heterosynaptic suppressions of GABA release. This suggests that these receptors may have evolved to monitor glutamate that has “spilled” out of the synapse. Thus, they may serve as the brain's evolutionary mechanism to prevent pathological changes in neuronal excitability and thus maintain homeostasis. Recent progress on the molecular and pharmacological aspects of these presynaptic mGlu receptors is unveiling their functions and the therapeutic directions of agents designed for these novel glutamate receptor targets.

Footnotes

  • Abbreviations:
    mGlu
    metabotropic glutamate
    GPCRs
    G-protein-coupled receptors
    CNS
    central nervous system
    GABA
    γ-aminobutyric acid
    EPSP
    excitatory postsynaptic potential
    MCPG
    α-methyl-carboxyphenylglycine
    5HT
    serotonin
    l-AP4
    l-2-amino-4-phosphonobutyric acid
    3,4-DCPG
    (S)3,4-dicarboxyphenyl glycine
    AMPA
    α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
    NMDA
    N-methyl-d-aspartate
    nRT
    thalamic reticular nucleus
    • Received April 3, 2001.
    • Accepted May 5, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 299 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 299, Issue 1
1 Oct 2001
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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Unveiling the Functions of Presynaptic Metabotropic Glutamate Receptors in the Central Nervous System

Darryle D. Schoepp
Journal of Pharmacology and Experimental Therapeutics October 1, 2001, 299 (1) 12-20;

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Research ArticlePERSPECTIVES IN PHARMACOLOGY

Unveiling the Functions of Presynaptic Metabotropic Glutamate Receptors in the Central Nervous System

Darryle D. Schoepp
Journal of Pharmacology and Experimental Therapeutics October 1, 2001, 299 (1) 12-20;
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  • Article
    • Abstract
    • Evolution of mGlu Receptors May Implicate Them as an Important Mechanism for Modulation of Neuronal Excitability
    • Modulation of Glutamatergic Functions by Group II mGlu Receptor Subtypes
    • Modulation of Glutamatergic Functions by Group III mGlu Receptor Subtypes
    • Modulation of Inhibitory Neurotransmission by Group II/III mGlu Receptors
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