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目的:研究维拉帕米(Ver)是否能抑制去甲肾上腺素(NE)诱导的培养大鼠心肌细胞β受体下调及其可能机制.方法:β受体密度用[3H]DNA放射配基标记法,细胞内游离钙用钙离子荧光探针Fura2AM法测定.结果:Ver能明显降低培养大鼠心肌细胞内游离钙水平,增加β受体密度;NE增加细胞内游离钙水平,降低β受体密度;Ver能明显抑制NE引起的细胞内游离钙增加和β受体密度的降低.结论:Ver能增加正常心肌细胞β受体密度,抑制NE产生的心肌β受体下调.
AIM: To investigate whether verapamil can inhibit the downregulation of β receptors in cultured rat cardiomyocytes induced by norepinephrine (NE) and its possible mechanism. Methods: The β receptor density was measured by [3H] DNA radioligand labeling method and intracellular free calcium was measured by Fura2AM method with calcium ion fluorescence probe. RESULTS: Ver significantly decreased intracellular free calcium levels and β receptor density in cultured rat myocardial cells; NE increased intracellular free calcium levels and decreased β receptor density; Ver significantly inhibited NE-induced intracellular free calcium increase and β Receptor density decreased. Conclusion: Ver increased the density of β receptor in normal cardiomyocytes and inhibited the down-regulation of β receptor in NE induced by NE.