GABAB receptor

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gamma-aminobutyric acid (GABA) B receptor, 1
Identifiers
Symbol GABBR1
Entrez 2550
HUGO 4070
OMIM 603540
RefSeq NM_021905
UniProt Q9UBS5
Other data
Locus Chr. 6 p21.3
gamma-aminobutyric acid (GABA) B receptor, 2
Identifiers
Symbol GABBR2
Alt. Symbols GPR51
Entrez 9568
HUGO 4507
OMIM 607340
RefSeq NM_005458
UniProt O75899
Other data
Locus Chr. 9 q22.1-22.3
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 for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels.[1] These receptors are found in the central and peripheral autonomic nervous system.[2]

Functions

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+.[2]

GABAB receptors are involved in behavioral actions of ethanol, [3] gamma-hydroxy butyric acid (GHB),[4] and possibly in pain.[5] Recent research suggests that these receptors may play an important developmental role. [6]

Structure

GABABRs are similar in structure to and in the same receptor family with metabotropic glutamate receptors.[7] There are two subtypes of the receptor, GABAB1 and GABAB2,[8][2] and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini.[2][7]

It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap.[2]

Agonists and antagonists

Image:GABA.png
GABA
Image:BaclofenStructure.png
Baclofen

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.

See also

References

  1. ↑ Chen K, Li H, Ye N, Zhang J, Wang J (2005). "Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro". Brain Res Bull 67 (4): 310-8. PMID 16182939.
  2. ↑ 2.0 2.1 2.2 2.3 2.4 Martin I.L., and Dunn S.M.J. 2002. "GABA Receptors". Tocris Cookson Ltd.
  3. ↑ Dzitoyeva S, Dimitrijevic N, Manev H (2003). "Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence". Proc Natl Acad Sci U S A 100 (9): 5485-90. PMID 12692303.
  4. ↑ Dimitrijevic N, Dzitoyeva S, Satta R, Imbesi M, Yildiz S, Manev H (2005). "Drosophila GABA(B) receptors are involved in behavioral effects of gamma-hydroxybutyric acid (GHB)". Eur J Pharmacol 519 (3): 246-52. PMID 16129424.
  5. ↑ Manev H, Dimitrijevic N (2004). "Drosophila model for in vivo pharmacological analgesia research". Eur J Pharmacol 491 (2-3): 207-8. PMID 15140638.
  6. ↑ Dzitoyeva S, Gutnov A, Imbesi M, Dimitrijevic N, Manev H (2005). "Developmental role of GABAB(1) receptors in Drosophila". Brain Res Dev Brain Res 158 (1-2): 111-4. PMID 16054235.
  7. ↑ 7.0 7.1 MRC (Medical Research Counsil). 2003. Glutamate receptors: Structures and functions. University of Brisotol Centre for Synaptic Plasticity.
  8. ↑ 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.

External links

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Transmembrane receptor: G protein-coupled receptors
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Class C: Metabotropic glutamate / pheromoneCalcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / SmoothenedFrizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened
uk:ГАМКB-рецептор




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Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .

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