Endogenous opiate peptides are considered to inhibit LH secretion via a dopaminergic mechanism, and increased opioid inhibition of LH secretion has been found in some hyperprolactinemic women with a pituitary microadenoma. To assess the role of endogenous dopaminergic tone in the opioid regulation of LH secretion in such patients, LH responses to an opioid antagonist (naloxone) and a dopamine antagonist (metoclopramide) were determined in 11 women with a prolactinoma. Neither naloxone nor metoclopramide administration induced any change in serum LH levels in normal women during the early follicular phase. In contrast, 7 of the 11 hyperprolactinemic women responded to both antagonists with a significant increase in LH levels. The parallelism in the LH responses to both antagonists in these hyperprolactinemic patients lends further support to a functional link between opioid and dopamine regulation of LH secretion.