Presynaptic agonist effect of phentolamine in the rabbit vas deferens and rat cerebral cortex.

Clonidine inhibited the electrically-induced twitch response of the rabbit and rat isolated vas deferens preparations and also the K+-evoked release of [3H]noradrenaline from rat cortical slices. This effect of clonidine was antagonized competitively by yohimbine. Phentolamine inhibited the electrically-induced twitch response of the rabbit, but not the rat, vas deferens and in low concentrations (less than 0.1 microM) also inhibited the K+-evoked release of [3H]NA from rat cortical slices. These inhibitory effects of phentolamine were antagonized by yohimbine in a competitive manner but were not antagonized by indoramin, an alpha 1-adrenoceptor antagonist. In the rabbit vas deferens, the effects of phentolamine were shown not to be due to the stimulation of beta-, H1-, H2-, 5-HT- or muscarinic receptors. These results are consistent with the view that phentolamine can act as an agonist at presynaptic alpha 2-adrenoceptors in the rabbit vas deferens and rat cortex but not in the rat vas deferens.