1. In rat aorta, 2,3-dibenzylbutane-1,4-diol (DBB) inhibited noradrenaline (NA)-induced contraction in a concentration-dependent manner. The inhibitory effect of DBB was observed in verapamil-pretreated muscle, and did not differ from that in the high K+ solution containing verapamil (1.0 microM). 2. DBB inhibited not only contraction, but [Ca2+]i elevation induced by NA (10 microM) with the same potency. 3. The inhibitory effect of DBB on NA-induced contraction was reversed by methylene blue (3.2 microM) and enhanced by M&B 22,948 (10 microM). 4. DBB (100 microM) alone increased cyclic GMP levels. This effect was attenuated by methylene blue (3.2 microM) and augmented by M&B 22,948 (10 microM). 5. From these results, the inhibitory effects of DBB on NA-induced contraction in rat aorta may be caused by an increase of cyclic GMP levels.