We have studied the in vitro effects of neurokinin A (NKA) on anterior pituitary GABA concentration and GABA release from the mediobasal hypothalamus and the neurointermediate lobe of male and ovariectomized female (OVX) rats. NKA significantly decreased the anterior pituitary GABA concentration, while the presence of a specific anti-NKA serum in the incubation medium increased the GABA concentration in this gland. By contrast, NKA did not modify basal or K(+)-evoked GABA release from the mediobasal hypothalamus of male or OVX rats. However, NKA decreased basal and K(+)-evoked GABA release from the neurointermediate lobe. Since GABA inhibits both prolactin (PRL) secretion from the anterior pituitary and the release of several putative PRL-releasing factors from the neurointermediate lobe, the decrease in anterior pituitary GABA concentration and the reduction in tubero-hypophyseal GABAergic activity induced by NKA may contribute to the stimulatory effect of this peptide on PRL secretion.