GABA, glutamate, and glycine release in the locus coeruleus were measured as a function of sleep/wake state in the freely-behaving cat using the microdialysis technique. GABA release was found to increase during rapid-eye-movement sleep as compared to waking values. GABA release during slow-wave sleep was intermediate between that of waking states and rapid-eye-movement sleep. The concentration of glutamate and glycine in microdialysis samples was unchanged across sleep and wake states. Our findings are consistent with the hypothesis that GABAergic inhibition is responsible for the cessation of discharge in locus coeruleus neurons during REM sleep. The data suggest that a population of GABAergic neurons innervating the locus coeruleus are selectively active during rapid-eye-movement sleep.