The neurotransmitter and andrenoceptors involved in the inhibition of luteinizing hormone (LH) release induced by stimulating the locus ceruleus nucleus (LC) have been characterized in ovariectomized, estrogen-primed rats in which the release of LH was triggered by electrical stimulation of the medial preoptic area. Blockade of norepinephrine synthesis by the injection of the dopamine beta-hydroxylase inhibitors, diethyldithiocarbamate or fusaric acid, prevented the inhibition of LH release, whereas blockade of epinephrine synthesis by injecting the phenylethanolamine N-methyltransferase inhibitor, 2,3-dichloro-methylbenzylamine, had no effect. In addition, the inhibition of LH release was prevented by systemic injection of propranolol but not of phenoxybenzamine. This inhibition was also suppressed in rats in which the ventral premammillary (PM) nucleus ipsilateral to the stimulated LC was lesioned, or in animals with a transverse cut placed just in front of the PM. A similar response was seen in rats in which propranolol but not phenoxybenzamine was applied to the PM ipsilateral to the stimulated LC. The present results indicate that norepinephrine, acting through beta-adrenoceptors mediates the transmission of impulses which, originating in the LC, inhibit the release of LH. The LC adrenergic fibers synapse in the PM before the neural information they convey is transfered to the gonadotropin-releasing hormone containing neurons.