The role of neurotransmitters in the release of prolactin (PRL) is reviewed. Special attention is paid to dopamine (DA) as the possible prolactin-inhibiting factor (PIF). Among other agents, estrogens alone can act directly on the pituitary galactotropes without involving hypothalamic factors. Peripherally, in addition to its stimulatory action on mammary tissue, PRL exerts a permissive role on ovarian steroidogenesis. A possible physiological action of this hormone on the regulation of adrenal function remains uncertain. The secretory rhythms of PRL are described and the mechanisms involved are discussed. A number of drugs can modify the secreting pattern of PRL mainly by acting on the dopaminergic control mechanisms. The usefulness of such agents in the clinical evaluation of galactotrope cell function is reviewed.