Abe A, Karaki H
Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan.
Jpn J Pharmacol. 1992 Dec;60(4):389-92. doi: 10.1254/jjp.60.389.
The inhibitory effect of 1,9-dideoxyforskolin (DFK) on the contraction of rat aorta was compared with that of forskolin. DFK inhibited the contraction induced by high K+ more strongly than that induced by norepinephrine, whereas forskolin more strongly inhibited the norepinephrine-induced contraction. The inhibitory effect of DFK on high K(+)-induced contraction was antagonized by an increase in extracellular Ca2+ concentration. DFK inhibited the increase in cytosolic Ca2+ level and contraction in parallel whereas forskolin inhibited the contraction more strongly than the cytosolic Ca2+ level. These results suggest that DFK, but not forskolin, inhibits vascular smooth muscle contraction by a Ca2+ channel blocker-like action.
将1,9 - 二脱氧福斯高林(DFK)对大鼠主动脉收缩的抑制作用与福斯高林进行了比较。DFK对高钾诱导的收缩的抑制作用比对去甲肾上腺素诱导的收缩更强,而福斯高林对去甲肾上腺素诱导的收缩抑制作用更强。细胞外钙离子浓度升高可拮抗DFK对高钾诱导收缩的抑制作用。DFK同时抑制细胞溶质钙离子水平升高和收缩,而福斯高林对收缩的抑制作用比对细胞溶质钙离子水平的抑制作用更强。这些结果表明,DFK而非福斯高林通过类似钙离子通道阻滞剂的作用抑制血管平滑肌收缩。