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首页> 外文期刊>BJU international >In vitro investigation of the bladder-vascular selectivity of levcromakalim and YM934 in human tissues.
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In vitro investigation of the bladder-vascular selectivity of levcromakalim and YM934 in human tissues.

机译：人体组织中左cromakalim和YM934的膀胱-血管选择性的体外研究。

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OBJECTIVE: To examine the potencies of the potassium-channel openers (KCOs) levcromakalim and YM934 as relaxing agents on human detrusor and human mesenteric artery smooth muscle, and to determine their bladder-vascular selectivity in vitro. MATERIALS AND METHODS: Strips of human detrusor muscle and mesenteric artery (with the endothelium removed) were set up in physiological salt solution and the tension developed by the tissues recorded. Tissues were precontracted with a concentration of carbachol (detrusor) or phenylephrine (artery) which caused 80% of maximal contraction, and relaxation responses to levcromakalim and YM934 were then obtained. RESULTS: Both KCOs caused relaxation of the bladder detrusor muscle and the mesenteric artery. Maximal responses, when plotted as a percentage of the precontraction, were greater for both KCOs in the bladder muscle than the artery, but the differences were small and not statistically significant. The sensitivity (drug potency) of the detrusor muscle to the KCOs was more than twice that of the artery but this selectivity was only statistically significant for YM934. CONCLUSIONS: Only minor bladder-vascular selectivity for levcromakalim and YM934 could be detected in vitro. This suggests that neither drug would be tolerated clinically, although the results suggest that further development of bladder-selective KCO agents appears feasible.
机译：目的：研究左旋cromakalim和YM934钾通道开放剂（KCOs）对人逼尿肌和肠系膜动脉平滑肌的作用，并测定其体外膀胱-血管选择性。材料与方法：在生理盐溶液中设置人类逼尿肌和肠系膜动脉的条带（去除内皮），并记录组织产生的张力。将组织预先加入一定浓度的卡巴胆碱（逼尿肌）或去氧肾上腺素（动脉），引起80％的最大收缩，然后获得对levcromakalim和YM934的松弛反应。结果：两个KCO均引起膀胱逼尿肌和肠系膜动脉松弛。当以收缩前百分比的形式绘制时，膀胱肌肉中的两个KCO的最大反应都比动脉大，但差异很小且无统计学意义。逼尿肌对KCO的敏感性（药物效力）是动脉的敏感性的两倍以上，但这种选择性对YM934仅具有统计学意义。结论：仅在体外可检测到左旋克马卡林和YM934的较小的膀胱-血管选择性。这表明这两种药物都不会在临床上被耐受，尽管结果表明进一步开发膀胱选择性KCO药物似乎是可行的。

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