GABAB receptor
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 |
GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels.[1] The changing potassium concentrations hyperpolarize the cell at the end of an action potential. The reversal potential of the GABAB-mediated IPSP is -100 mV, which is much more hyperpolarized than the GABAA IPSP. GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system.[citation needed]
Contents
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 voltage-gated sodium channels from opening, action potentials from firing, and VDCCs from opening, and so stops neurotransmitter release.[citation needed] Thus GABAB receptors are considered inhibitory receptors.[by whom?]
GABAB receptors can also reduce the activity of adenylyl cyclase and decrease the cell’s conductance to Ca2+.[citation needed]
GABAB receptors are involved in behavioral actions of ethanol,[2] gamma-Hydroxybutyric acid (GHB),[3] and possibly in pain.[4] Recent research suggests that these receptors may play an important developmental role.[5]
Structure
GABAB Receptors are similar in structure to and in the same receptor family with metabotropic glutamate receptors.[6] There are two subtypes of the receptor, GABAB1 and GABAB2,[7] and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini.[6]
It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap.[citation needed]
Ligands
Agonists
- GABA
- 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.
- gamma-Hydroxybutyrate (GHB)
- Phenibut
- Isovaline
- 3-Aminopropylphosphinic acid
- Lesogaberan
- SKF-97541: 3-Aminopropyl(methyl)phosphinic acid, 10x more potent than baclofen as GABAB agonist, but also GABAC antagonist
- CGP-44532
Positive Allosteric Modulators
Antagonists
- Homotaurine [12]
- Ginsenosides [13]
- 2-OH-saclofen
- Fasoracetam
- Saclofen
- Phaclofen
- SCH-50911
- 2-Phenethylamine
- CGP-35348
- CGP-52432: 3-([(3,4-Dichlorophenyl)methyl]amino]propyl) diethoxymethyl)phosphinic acid, CAS# 139667-74-6
- CGP-55845: (2S)-3-([(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl)(phenylmethyl)phosphinic acid, CAS# 149184-22-5
- SGS-742 [14][15]
See also
References
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External links
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- ↑ 6.0 6.1 MRC (Medical Research Council). 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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- Pages with reference errors
- Genes on human chromosome 6
- Genes on human chromosome 9
- Articles with unsourced statements from February 2014
- Articles with unsourced statements from October 2015
- Articles with specifically marked weasel-worded phrases from May 2016
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- G protein coupled receptors