Zhang X Q, Watanabe Y, Ohnishi M, Baba T, Shibuya T
Department of Pharmacology, Tokyo Medical College, Japan.
Jpn J Pharmacol. 1993 Aug;62(4):411-4. doi: 10.1254/jjp.62.411.
The inhibitory effects of calcium antagonists on high-potassium or glutamate (Glu) enhanced intracellular calcium ion ([Ca2+]i) levels were studied in cultured cerebellar granule cells. Dosages between 0.5 and 10 microM of flunarizine, nicardipine, SM6586 and SM12565 reduced the rise in [Ca2+]i induced by 50 mM KCl in a dose-dependent manner, although diltiazem, verapamil and nifedipine showed less effects on such [Ca2+]i increases. SM6586, SM12565 and flunarizine at dosages below 10 microM each reduced the magnitude of the [Ca2+]i increase induced by 25 microM Glu, but the other examined calcium antagonists were less effective. These results suggest the dissimilar efficacy of calcium antagonists on the inhibition of [Ca2+]i levels increased by high-potassium and Glu.
在培养的小脑颗粒细胞中研究了钙拮抗剂对高钾或谷氨酸(Glu)增强的细胞内钙离子([Ca2+]i)水平的抑制作用。0.5至10微摩尔的氟桂利嗪、尼卡地平、SM6586和SM12565剂量以剂量依赖方式降低了50毫摩尔氯化钾诱导的[Ca2+]i升高,尽管地尔硫卓、维拉帕米和硝苯地平对这种[Ca2+]i增加的作用较小。剂量低于10微摩尔的SM6586、SM12565和氟桂利嗪各自降低了25微摩尔Glu诱导的[Ca2+]i增加幅度,但其他检测的钙拮抗剂效果较差。这些结果表明钙拮抗剂对抑制高钾和Glu增加的[Ca2+]i水平具有不同的功效。