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

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]

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

GABA
GHB
Lesogaberan

Agonists

CGP-7930

Positive Allosteric Modulators

Phaclofen
SCH-50911

Antagonists

See also

References

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  6. ↑ 6.0 6.1 MRC (Medical Research Council). 2003. Glutamate receptors: Structures and functions. University of Brisotol Centre for Synaptic Plasticity.
  7. ↑ 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.
  8. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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External links

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