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首页> 外文期刊>Life sciences >Screening for novel drug effects with a microphysiometer: a potent effect of clofilium unrelated to potassium channel blockade.
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Screening for novel drug effects with a microphysiometer: a potent effect of clofilium unrelated to potassium channel blockade.

机译：用微生理仪筛选新药的作用：与钾离子通道阻滞无关的clofilium的有效作用。

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摘要

Changes in cellular metabolism in response to pharmacological compounds can be detected using a biosensor known as a microphysiometer, which measures the rate at which cells release acidic metabolites. We have applied this technique to screen for effects of cation channel blockers on the metabolism of a variety of human and murine cell lines. At concentrations sufficient for cation channel blockade, most of these drugs have little or no effect on cellular metabolism as measured by acid release. In contrast, the potassium channel blocker clofilium triggers sustained increases in acid release at low (> or = 3 microM) concentration. Acid release persists in media containing high (150 mM) extracellular potassium. This release is not triggered by chemically similar potassium channel blockers. Thus these metabolic effects reflect a potent and specific function of clofilium which is unrelated to potassium channel blockade. Attempts to identify physiological correlates to this response revealed that low concentrations of clofilium but not other potassium channel blockers cause lymphoma apoptosis. These findings demonstrate that effects of clofilium found in other studies may not be due to changes in plasma membrane potassium conductance.
机译：可以使用称为微生理仪的生物传感器检测响应药理化合物的细胞代谢变化，该传感器可测量细胞释放酸性代谢物的速率。我们已将此技术应用于筛选阳离子通道阻滞剂对多种人和鼠细胞系代谢的影响。在足够的阳离子通道阻断浓度下，这些药物中的大多数对细胞代谢的影响很小或没有影响，通过酸释放来衡量。相反，钾通道阻滞剂clofilium在低（>或= 3 microM）浓度下触发酸释放的持续增加。酸释放在含有高（150 mM）细胞外钾的培养基中持续存在。这种释放不是由化学相似的钾通道阻滞剂触发的。因此，这些代谢作用反映出与钾离子通道阻滞无关的clofilium的有效和特定功能。试图确定与此反应有生理相关性的尝试表明，低浓度的clofilium（而非其他钾通道阻滞剂）会导致淋巴瘤凋亡。这些发现表明，在其他研究中发现的clofilium的作用可能不是由于质膜钾电导的变化。

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