GABA-B RECEPTORS - ROLE AND THERAPEUTIC IMPLICATIONS IN CNS DISORDERS

The neurotransmitter gamma-aminobutyric acid (GABA) activates more tha n one receptor subtype, including the metabotropic receptor, GABA(B). GABA(B) receptors are located at pre- and postsynaptic sites on centra l neurons and mediate changes in the membrane conductance of potassium and calcium ions. This influences transmitter release as well as affe cting neuronal activity directly. The GABA(B) system can be modified b y receptor ligands. This is currently exploited clinically, within the spinal cord, with the use of the GABA(B) agonist baclofen to treat sp asticity and, to a lesser degree, trigeminal neuralgia. However, other potential uses of GABA(B) ligands may be on the horizon in relation t o absence epilepsy, cognitive impairment and depression.