首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Effect of milrinone analogues on intracellular calcium increase in single living H9C2 cardiac cells.
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Effect of milrinone analogues on intracellular calcium increase in single living H9C2 cardiac cells.

机译:米力农类似物对单个活H9C2心脏细胞内细胞内钙增加的影响。

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摘要

The synthesis of milrinone analogues where the 4-pyridyl moiety was replaced by an ester or amide group is reported. Only amide derivatives are able to support intracellular calcium influx following chemical depolarization with 60 mM KCl in a percentage varying from 20 to 45% of differentiated H9C2 cardiomyocytes. Those cells were differentiated after chronic exposure to 10 nM retinoic acid which induces the expression of voltage-gated calcium channels. Analogues of milrinone containing an ester function did not show significant activity.
机译:报道了米力农酮类似物的合成,其中4-吡啶基部分被酯或酰胺基团取代。用60 mM KCl进行化学去极化后,只有酰胺衍生物能够支持细胞内钙内流,其百分比在分化的H9C2心肌细胞的20%到45%之间。长期暴露于10 nM视黄酸会诱导分化,诱导电压门控钙通道的表达。含酯功能的米力农的类似物未显示出明显的活性。

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