New compounds SIPI5052 in vitro function of blood vessel contraction.doc

 PAGE \* MERGEFORMAT 11 New compounds SIPI5052 in vitro function of blood vessel contraction 【Abstract】 Objective To understand the anti-cerebral ischemia SIPI5052 whether a new compound of calcium antagonism, the observation of its norepinephrine or potassium-induced vasoconstriction in vitro function. The introduction of machine-based measurement system in vitro vascular function observed SIPI5052 on isolated rat thoracic aorta, rabbit thoracic aorta and mesenteric artery systolic function. The results could significantly inhibit the subjects SIPI5052 vascular norepinephrine or potassium-induced contraction responses in a dose-dependent. Blood vessels in rats, the onset of the concentration of 3 × 10-6mol / L, IC50 of 1.66 × 10-4mol / L, 100% inhibitory concentration of 3 × 10-3mol / L. In rabbit blood vessels, the onset of the concentration of 3 × 10-4mol / L, IC50 of 4.17 × 10-4 ~ 5.37 × 10-4mol / L, 100% inhibitory concentration ≥ 3 × 10-3mol / L. Conclusion SIPI5052 with calcium antagonism. Vascular response of SIPI5052 sensitive than the rabbit blood vessels. Antagonistic effect of calcium is likely to be the anti-cerebral ischemia SIPI5052 one of the mechanisms. Keywords: piperazines; aorta; mesenteric artery; contraction reaction; calcium channel; anti-cerebral ischemia Effect of SIPI5052, a new chemical entity, on the contraction of isolated arteries 【Abstract】 Objective To study the effect of a new anti-stroke chemical entity SIPI5052 on Ca2 channels, by observing its effect on norepinephrine or KCl induced contraction in isolated blood vessels.Methods Using IOX computerized system (EMKA Technologies, Paris, France) to record the changes of isometric tension in isolated rat aorta, rabbit aorta and rabbit mesenteric artery.Results SIPI5052 can significantly inhibit norepinephrine or KCl induced contraction in the examined blood vessels and the effect is concentration-dependent. minimum inhibitory concentration in rat ao