Résumé
The effects of C1-930, a known selective phosphodiesterase 111 inhibitor, on vascular resistance and rat aortic strip contraction were studied CI-930 025mg/kg injected into the perfused artery, reduced vascular resistance markedly in femoral artery and internal carotid artery in anaesthetized rats. The action lasted for about 15-20 min. CI-930 in vitro inhibited norepinephrine (NE) and TXA2/PGH, mimetic U-46619 induced rat aortic strip contraction significantly with PD, values of 6.71 and 5.5 respectively. The inhibitory effects of CI-930 on NE and U-46619 induced contraction were more potent than that of KG induced contraction. CI-930 0.01 - 10?mol/L exhibited a potential inhibitory effects on intracellular Ca2+ dependent contraction of rat aortic strip induced by NE, but had no effect on extracellular Ca2+ dependent contraction. The results suggest that CI-930 can possess a potent intracellular Ca2+ dependent vasodilating effects in vitro and in vivo.