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Metabotropic glutamate 1 receptor: current concepts and perspectives
Francesco Ferraguti1, Luca Crepaldi, Ferdinando Nicoletti
1Department of Pharmacology, Innsbruck Medical University, Peter-Mayr Strasse 1a, Innsbruck A-6020, Austria. francesco.ferraguti@i-med.ac.at
Pharmacological Reviews
|December 30, 2008
Summary
Metabotropic glutamate (mGlu) receptors, particularly mGlu1, are crucial G-protein coupled receptors. Research clarifies their roles in neuronal systems and potential for treating neurological and psychiatric disorders.
Area of Science:
- Neuroscience
- Molecular Biology
- Pharmacology
Background:
- Metabotropic glutamate (mGlu) receptors are G-protein coupled receptors activated by glutamate.
- Eight mGlu receptor subtypes have been identified, encoded by distinct genes.
- mGlu1 receptor, the first cloned, is extensively studied and prototypical.
Purpose of the Study:
- To review advancements in mGlu1 receptor pharmacology and intracellular transduction.
- To elucidate the pathophysiological role of mGlu1 receptors.
- To consider the therapeutic potential of mGlu1 receptor modulation for neurological and psychiatric disorders.
Main Methods:
- Biochemical, anatomical, physiological, and pharmacological investigations.
- Analysis of alternatively spliced variants of mGlu1 receptors.
- Application of genetic approaches and selective antagonists.
Main Results:
- mGlu1 receptors, with subtype 5, couple to phospholipase C and mobilize intracellular Ca(2+).
- Alternative splicing affects mGlu1 receptor C-terminal domains and localization.
- Genetic and pharmacological tools aid in clarifying mGlu1 receptor functions in neuronal systems.
Conclusions:
- Recent findings enhance understanding of mGlu1 receptor pharmacology, signaling, and function.
- mGlu1 receptors play significant roles in various neuronal systems.
- Targeting mGlu1 receptors offers potential for novel therapeutic strategies in neurological and psychiatric conditions.
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