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]


Wikimedia Foundation. 2010.

Игры ⚽ Поможем сделать НИР

Look at other dictionaries:

  • GABAB — GABA Rezeptoren sind Transmembranproteine in Nervenzellen, die spezifisch den Neurotransmitter γ Aminobuttersäure (GABA) binden. Es gibt ionotrope und metabotrope GABA Rezeptoren. Zu den ionotropen Rezeptoren zählen der GABAA und der GABAC… …   Deutsch Wikipedia

  • GABAB — gamma aminobutyric acid ionotropic receptor family B …   Medical dictionary

  • GABAB — • gamma aminobutyric acid ionotropic receptor family B …   Dictionary of medical acronyms & abbreviations

  • GABA receptor — The GABA receptors are a class of receptors that respond to the neurotransmitter γ aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are three classes of GABA receptors: GABAA, GABAB,… …   Wikipedia

  • GABAA receptor — The GABAA receptor is one of two ligand gated ion channels responsible for mediating the effects of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the brain. In addition to the GABA binding site, the GABAA receptor… …   Wikipedia

  • GABAC receptor — protein Name = gamma aminobutyric acid (GABA) receptor, rho 1 caption = width = HGNCid = 4090 Symbol = GABRR1 AltSymbols = EntrezGene = 2569 OMIM = 137161 RefSeq = NM 002042 UniProt = P24046 PDB = ECnumber = Chromosome = 6 Arm = q Band = 14… …   Wikipedia

  • GABA receptor — Member of a family of receptors for neurotransmitters that includes those for glycine and the nicotinic acetylcholine receptor. Opened by g amino butyric acid (GABA). There are two main classes; GABA A and GABAC receptors are ionotropic, GABAB… …   Dictionary of molecular biology

  • Metabotropic receptor — is a subtype of membrane receptors at the surface or in vesicles of eukaryotic cells. In the nervous system, based on their structural and functional characteristics, neurotransmitter receptors can be classified into two broad categories:… …   Wikipedia

  • G protein-coupled receptor — G protein coupled receptors (GPCRs), also known as seven transmembrane domain receptors, 7TM receptors, heptahelical receptors, and G protein linked receptors (GPLR), comprise a large protein family of transmembrane receptors that sense molecules …   Wikipedia

  • Gamma-Hydroxybutyric acid — γ Hydroxybutyric acid Systematic (IUPAC) name 4 Hydroxybutanoic acid …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”