The role of GABA(B) receptors in the regulation of excitatory neurotransmission.

Abstract

GABA(B) receptors are the metabotrophic receptors for GABA. They are members of the G-protein coupled superfamily of receptors but are highly unusual as they are made up of a dimer of 7-transmembrane spanning subunits. The receptors are widely distributed throughout the central nervous system where they act post-synaptically to cause a long-lasting hyperpolarisation through the activation of a potassium conductance. They are also present pre-synaptically where they act as auto and heteroreceptors to inhibit neurotransmitter release. GABA(B) receptors play a complex role in the regulation of excitatory transmission and their activation can have both inhibitory and dis-inhibitory effects. This has profound physiological and behavioural consequences including modification of LTP and memory, regulation of seizure activity and nociception.