We examined the effects of gamma-aminobutyric acid (GABA) and naloxone, a potent opioid antagonist, on arginine vasopressin (AVP) secretion in conscious rats in order to study the relationship of GABA and endogenous opioid peptides in the regulation of AVP secretion. Intracerebroventricular administration of GABA caused a time- and dose-dependent decrease in the plasma concentration of AVP that was elevated by hypertonic saline injection, whereas it did not affect the basal AVP. Pretreatment with naloxone (10 mg/kg) significantly attenuated the inhibitory effect of GABA (100 micrograms) on AVP release. These results suggest that GABA produces an inhibition of AVP release stimulated by hypertonic saline, and that this inhibitory effect may be mediated at least in part by the endogenous opioid systems.