GABAB receptor

GABAB receptor

protein
Name= gamma-aminobutyric acid (GABA) B receptor, 1
caption=


width=
HGNCid=4070
Symbol=GABBR1
AltSymbols=
EntrezGene=2550
OMIM=603540
RefSeq=NM_021905
UniProt=Q9UBS5
PDB=
ECnumber=
Chromosome=6
Arm=p
Band=21.3
LocusSupplementaryData=
protein
Name= gamma-aminobutyric acid (GABA) B receptor, 2
caption=


width=
HGNCid=4507
Symbol=GABBR2
AltSymbols=GPR51
EntrezGene=9568
OMIM=607340
RefSeq=NM_005458
UniProt=O75899
PDB=
ECnumber=
Chromosome=9
Arm=q
Band=22.1
LocusSupplementaryData=-22.3

GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels.cite journal |author=Chen K, Li H, Ye N, Zhang J, Wang J |title=Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro |journal=Brain Res Bull |volume=67 |issue=4 |pages=310–8 |year=2005 |pmid=16182939 |doi=10.1016/j.brainresbull.2005.07.004] These receptors are found in the central and peripheral autonomic nervous system.Martin I.L., and Dunn S.M.J. 2002. [http://www.tocris.com/pdfs/gabarev.pdf GABA receptors] Tocris Cookson Ltd. ]

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+. ]

GABAB receptors are involved in behavioral actions of ethanol, [cite journal |author=Dzitoyeva S, Dimitrijevic N, Manev H |title=Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence |journal=Proc Natl Acad Sci U S A |volume=100 |issue=9 |pages=5485–90 |year=2003 |pmid=12692303 |doi=10.1073/pnas.0830111100] gamma-Hydroxybutyric acid (GHB), [cite journal |author=Dimitrijevic N, Dzitoyeva S, Satta R, Imbesi M, Yildiz S, Manev H |title=Drosophila GABA(B) receptors are involved in behavioral effects of gamma-hydroxybutyric acid (GHB) |journal=Eur J Pharmacol |volume=519 |issue=3 |pages=246–52 |year=2005 |pmid=16129424 |doi=10.1016/j.ejphar.2005.07.016] and possibly in pain. [cite journal |author=Manev H, Dimitrijevic N |title=Drosophila model for in vivo pharmacological analgesia research |journal=Eur J Pharmacol |volume=491 |issue=2-3 |pages=207–8 |year=2004 |pmid=15140638 |doi=10.1016/j.ejphar.2004.03.030] Recent research suggests that these receptors may play an important developmental role. [cite journal |author=Dzitoyeva S, Gutnov A, Imbesi M, Dimitrijevic N, Manev H |title=Developmental role of GABAB(1) receptors in Drosophila |journal=Brain Res Dev Brain Res |volume=158 |issue=1-2 |pages=111–4 |year=2005 |pmid=16054235 |doi=10.1016/j.devbrainres.2005.06.005]

Structure

GABABRs are similar in structure to and in the same receptor family with metabotropic glutamate receptors.MRC (Medical Research Council). 2003. [http://www.bris.ac.uk/Depts/Synaptic/info/glutamate.html Glutamate receptors: Structures and functions.] University of Brisotol Centre for Synaptic Plasticity.] There are two subtypes of the receptor, GABAB1 and GABAB2, [Purves D., Augustine G.J., Fitzpatrick D., Katz L.C., LaMantia A.S., McNamara J.O., and Williams S.M. 2001. [http://www.ncbi.nlm.nih.gov/books/bv.fcgi?rid=neurosci.chapter.469 "Neuroscience", Second Edition.] Sinauer Associates, Inc.] ] and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini. ] ]

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

Agonists and antagonists

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

* GABA receptor
* GABAA receptor
* GABAC receptor

References

External links

* [http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1276 IUPHAR GPCR Database - GABAB Receptors]


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