Vasorelaxant and antihypertensive effects of ZCM298, a dihydropyridine derivative, are through inhibiting extracellular calcium influx

作者: Li-Xin Zhang , Xin-lin Chen , Peng-bo Yang , San-Qi Zhang , Yong-Xiao Cao

DOI: 10.1016/S1734-1140(13)70965-4

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摘要: Abstract Background ZCM298 is a novel 1,4-dihydropyridine derivative. The aim of the study was to investigate its vasodilation and hypotension, related mechanisms. Methods isometric tension artery ring segments recorded using an in vitro myography system. blood pressure spontaneously hypertensive rats (SHRs) measured vivo non-invasive tail cuff Changes intracellular calcium concentration ([Ca 2+ ] i ) mesenteric were surveyed real-time confocal microscopy. Regional cerebral flow (rCBF) pia mater monitored by laser-Doppler flowmetry (LDP). Results (10 −9 –10 −4 M) relaxed rat obviously concentration-dependently, which not affected removal endothelium. shifted concentration-contractile curves arteries response phenylephrine, U46619, KCl CaCl 2 towards right non-parallel manner. potency on relaxing basilar much higher than artery. did depress phenylephrine-induced vasoconstriction; however, it inhibited contraction caused addition Ca -free solution. −6 increase [Ca ]i induced improved rCBF at 0.03 0.06 mg/kg. depressed systolic diastolic SHRs dose-dependent Conclusions relaxes probably through inhibiting extracellular influx decreases SHRs. more potent improves rats.

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