GABAB Receptors

SummaryThe neurotransmitter γ-aminobutyric acid (GABA) activates more than one receptor subtype, including the metabotropic receptor, GABAB. GABAB receptors are located at pre- and postsynaptic sites on central neurons and mediate changes in the membrane conductance of potassium and calcium ions. This influences transmitter release as well as affecting neuronal activity directly.The GABAB system can be modified by receptor ligands. This is currently exploited clinically, within the spinal cord, with the use of the GABAB agonist baclofen to treat spasticity and, to a lesser degree, trigeminal neuralgia. However, other potential uses of GABAB ligands may be on the horizon in relation to absence epilepsy, cognitive impairment and depression.