To clarify the role of endogenous opioid peptides in the control of vasopressin (AVP) secretion, the effects of an endogenous kappa-agonist, leumorphin, derived from proenkephalin B and an opioid antagonist, naloxone, on AVP secretion were examined in conscious and freely moving rats. Intraperitoneal injection of nicotine markedly increased AVP secretion in rats. The nicotine-induced AVP secretion was significantly suppressed by intracerebroventricular (i.c.v.) pretreatment with leumorphin. Intravenous injection of naloxone significantly increased the basal AVP level and carbachol-induced AVP secretion. These results indicate that endogenous opioid peptides have an inhibitory effect on AVP secretion in rats.