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GABAB receptor - Wikipedia, the free encyclopedia

GABAB receptor

From Wikipedia, the free encyclopedia

The correct title of this article is GABAB receptor. It features superscript or subscript characters that are substituted or omitted because of technical limitations.

GABAB receptors (GABABR) are metabotropic transmembrane receptors that are linked via G-proteins to potassium channels (Chen et al., 2005). These receptors are found in the central and peripheral autonomic nervous system (Martin and Dunn, 2002). They can stimulate the opening of K+ channels which brings the neuron closer to the equilibrium potential of K+, hyperpolarising the neuron. This prevents sodium channels from opening, action potentials from firing, and VDCCs from opening, and so stops neurotransmitter release. Thus GABAB receptors are considered inhibitory receptors.

GABAB receptors can also reduce the activity of adenylyl cyclase and decrease the cell’s conductance to Ca2+ (Siegel et al., 1999; Martin and Dunn, 2002).

GABAB receptors are involved in behavioral actions of ethanol [1], gamma-hydroxy butyric acid (GHB)[2], and possibly in pain [3]. Recent research suggests that these receptors may play an important developmental role [4].

GABABRs are similar in structure to and in the same receptor family with metabotropic glutamate receptors (MRC, 2003). There are two subtypes of the receptor, GABAB1 and GABAB2 (Purves et al., 2001; Martin and Dunn, 2002), and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini (Martin and Dunn, 2002; MRC, 2003). It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap (Martin and Dunn, 2002).

Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy. Saclofen, phaclofen and SCH-50911 are selective GABAB antagonists.

[edit] See also

[edit] References

  • Chen K., Lia H.Z., Yea N., Zhanga J., and Wang J.J. 2005. Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Research Bulletin, 67(4), 310-318.
  • Kandel ER, Schwartz JH, Jessell TM. Principles of Neural Science, 4th ed. pp.178-180. McGraw-Hill, New York (2000). ISBN 0-8385-7701-6
  • Martin I.L., and Dunn S.M.J. 2002. "GABA Receptors". Tocris Cookson Ltd.
  • MRC (Medical Research Counsil). 2003. Glutamate receptors: Structures and functions. University of Brisotol Centre for Synaptic Plasticity.
  • Purves D., Augustine G.J., Fitzpatrick D., Katz L.C., LaMantia A.S., McNamara J.O., and Williams S.M. 2001. Neuroscience, Second Edition. Sinauer Associates, Inc.

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