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GABA(B) receptors as potential therapeutic targets
Claire-Marie Vacher1, Bernhard Bettler
1Pharmazentrum, University of Basel, Department of Physiology, Klingelbergstr. 50-70, CH-4056 Basel, Switzerland. bernhard.bettler@unibas.ch
Current Drug Targets. CNS and Neurological Disorders
|July 23, 2003
Summary
Gamma-Aminobutyric acid-B (GABA(B)) receptors are key drug targets for neurological disorders. Research advances in understanding GABA(B) receptor function and allosteric drugs offer new therapeutic possibilities.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- Gamma-Aminobutyric acid-B (GABA(B)) receptors are widely distributed in the nervous system and linked to various neurological and psychiatric conditions.
- Current GABA(B) agonist (baclofen) use is limited by side effects and tolerance; antagonists face challenges like poor brain penetration and proconvulsive effects.
- The cloning of GABA(B) receptors in 1997 spurred research into developing safer and more selective therapeutic agents.
Purpose of the Study:
- To provide an updated overview of GABA(B) receptor molecular composition, physiology, and pharmacology.
- To discuss how current knowledge impacts ongoing and future drug discovery efforts for GABA(B) receptor-targeted therapies.
- To explore the therapeutic potential of GABA(B) receptors, considering recent insights into their function and allosteric modulation.
Main Methods:
- Review of recent scientific literature on GABA(B) receptor research.
- Analysis of findings from gene knockout mouse models to identify key neuronal systems.
- Exploration of the relationship between GABA(B) receptors and gamma-hydroxybutyrate (GHB) receptors.
Main Results:
- GABA(B) receptors require heteromerization for function, providing insights into G-protein coupled receptor structure and enabling the identification of allosteric drugs.
- Gene knockout studies identified neuronal systems under tonic GABA(B) control, indicating optimal targets for therapeutic intervention.
- Significant progress has been made in understanding the interplay between GABA(B) receptors and GHB receptors.
Conclusions:
- Advances in understanding GABA(B) receptor structure and function have paved the way for developing more selective and safer drugs.
- Targeting neuronal systems under tonic GABA(B) control presents a promising therapeutic strategy for various disorders.
- Continued research into GABA(B) receptor pharmacology and physiology is crucial for advancing drug discovery and clinical applications.