A Novel Gaba Receptor on Central Neurones

The features of γ-aminobutyric acid (GABA) as an inhibitory neurotransmitter are described, together with those of its receptor as defined by both iontophoretic and radiolabelled ligand binding techniques. Evidence is presented supporting the existence of a second GABA receptor at both peripheral nerve endings and within the CNS. At the classical receptor, GABA can produce a depolarisation of the ganglion cell body or mediate hyperpolarisation within the CNS by increasing membrane conductance to chloride ions. At this second receptor GABA acts in a bicuculline-insensitive manner to reduce neurotransmitter outflow.

Many GABA analogues active at the classical receptor are inactive at the second receptor but by contrast baclofen which is inactive at the classical receptor is a potent agonist at the novel site.