The effects of a phorbol ester, 12-deoxyphorbol 13-isobutyrate (DPB), on contraction of isolated vascular smooth muscle of rat aorta were examined. DPB (100 nM-1 microM) induced a concentration-dependent contraction in resting aorta. DPB (3-100 nM) also induced a concentration-dependent relaxation of the norepinephrine-induced contraction. The contractile effect of DPB was potentiated whereas the relaxant effect was inhibited by endothelium removal or by methylene blue, suggesting that lower concentrations of DPB release endothelium-derived relaxing factor to inhibit contraction in rat aorta.