GABA B receptor
GABAB Receptor[edit | edit source]
The GABAB receptor is a type of GABA receptor that is metabotropic, meaning it is a G-protein coupled receptor (GPCR). It is one of the two main types of receptors for gamma-aminobutyric acid (GABA), the primary inhibitory neurotransmitter in the central nervous system (CNS). Unlike the ionotropic [[GABAA receptor]], which directly mediates fast synaptic inhibition, the GABAB receptor mediates slower, prolonged inhibitory signals.
Structure[edit | edit source]
The GABAB receptor is a heterodimer composed of two subunits: GABAB1 and GABAB2. These subunits are necessary for the receptor's function and are linked together to form a functional receptor complex. The GABAB1 subunit is responsible for binding GABA, while the GABAB2 subunit is essential for G-protein coupling and signal transduction.
Mechanism of Action[edit | edit source]
Upon binding of GABA to the GABAB receptor, a conformational change occurs, activating the associated G-proteins. This activation leads to the inhibition of adenylate cyclase, a decrease in cyclic AMP (cAMP) levels, and the opening of potassium channels while closing calcium channels. The result is hyperpolarization of the neuron, making it less likely to fire an action potential, thus exerting an inhibitory effect.
Physiological Role[edit | edit source]
GABAB receptors are widely distributed in the brain and spinal cord. They play a crucial role in modulating synaptic transmission, neuronal excitability, and synaptic plasticity. These receptors are involved in various physiological processes, including:
- Regulation of neurotransmitter release
- Modulation of pain perception
- Control of muscle tone
- Influence on cognitive function and memory
Clinical Significance[edit | edit source]
GABAB receptors are implicated in several neurological and psychiatric disorders. Dysregulation of GABAB receptor function has been associated with conditions such as:
Pharmacology[edit | edit source]
Agonists and antagonists of the GABAB receptor are of significant interest in pharmacology. Baclofen, a GABAB receptor agonist, is used clinically as a muscle relaxant and in the treatment of spasticity. Research is ongoing to develop more selective drugs targeting these receptors for therapeutic purposes.
See Also[edit | edit source]
- [[GABAA receptor]]
- Neurotransmitter
- Central nervous system
References[edit | edit source]
- Bowery, N. G., & Enna, S. J. (2000). "Gamma-aminobutyric acidB receptors: first of the functional metabotropic heterodimers." *Journal of Pharmacology and Experimental Therapeutics*, 292(1), 2-7.
- Bettler, B., Kaupmann, K., Mosbacher, J., & Gassmann, M. (2004). "Molecular structure and physiological functions of GABAB receptors." *Physiological Reviews*, 84(3), 835-867.
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