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Effects of(1R,9S)-beta-Hydrastine on Intracellular Calcium Concentration in PC12 Cells

机译:(1R,9S)-β-羟基对PC12细胞内钙离子浓度的影响

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(1R,9S)-beta-Hydrastine(BHS)decreases the basal intracellular Ca~(2+)concentration([Ca~(2+)]_i)in PC12 cells.~(5))This study examined the effects of(1R,9S)-BHS on [Ca~(2+)]_i in PC12 cells.(1R,9S)-BHS at 10-100 flu in combination with a high extracellular K~+ level(56 mM)inhibited the release of dopamine in a concentration-dependent manner with an IC_(50)value of 66.5mu M.BHS at 100 mu M inhibited the sustained increase in [Ca~(2+)]_i induced by a high K~+ level(56 m M),and had an inhibitory effect on the 2 mu M nifedipine-induced blockage of the K~+-stimulated sustained increase in [Ca~(2+)]_i.In addition,(1R,9S)-BHS at 100 mu M prevented the rapid and sustained increase in [Ca~(2+)]_i elicited by 20 mM caffeine,but did not have an effect on the increase induced by 1 mu M thapsigargin,in the presence of external Ca~(2+).These results suggest that the active sites of(1R,9S)-BHS are mainly L-type Ca~(2+)channels and caffeine-sensitive Ca~(2+)-permeable channels in PC12 cells.
机译:(1R,9S)-β-Hydrastine(BHS)降低PC12细胞中基础细胞内Ca〜(2+)浓度([Ca〜(2 +)] _ i)。〜(5)) PC12细胞中[Ca〜(2 +)] _ i上的1R,9S)-BHS。10-100flu的(1R,9S)-BHS与高细胞外K〜+水平(56 mM)结合抑制多巴胺浓度依赖性,IC_(50)值为66.5μM。BHS在100μM时抑制了高K〜+水平(56 m M)引起的[Ca〜(2 +)] _ i持续增加),并抑制2μM硝苯地平对K〜+刺激的[Ca〜(2 +)] _ i持续增加的阻滞作用。此外,(1R,9S)-BHS在100μM时抑制了20 mM咖啡因引起的[Ca〜(2 +)] _ i的快速和持续增加,但在外部Ca〜(2+)存在的情况下,对1μM毒胡萝卜素诱导的增加没有影响。这些结果表明,(1R,9S)-BHS的活性位点主要是PC12细胞中的L型Ca〜(2+)通道和咖啡因敏感的Ca〜(2+)可透过通道。

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