Norbormide: a calcium entry blocker with selective vasoconstrictor activity in rat peripheral arteries.

S. Bova, L. Cima, V. Golovina, S. Luciani, G. Cargnelli
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引用次数: 17

Abstract

Norbormide is a unique vasoactive substance endowed with species- and tissue-specific, endothelium independent, vasoconstrictor activity that is restricted to the peripheral arteries of rat. In rat aorta and in all tested arteries of other species norbormide exhibits vasorelaxant property presumably due to the blockade of calcium channels. A calcium entry blocker effect of norbormide has also been described in isolated, perfused guinea pig hearts. In these preparations norbormide produced coronary vasodilator, as well as negative inotropic and dromotropic effects. In single ventricular myocytes of guinea pigs norbormide reduces L-type calcium current. The mechanism underlying the selective vasoconstrictor effect of norbormide is unknown. In rat caudal artery, a vessel contracted by norbormide, the drug activates phospholipase C (PLC) signal cascade which is the biochemical pathway involved in the contractile effect triggered by most receptor-activating vasoactive agents. Therefore, norbormide-induced contraction of rat peripheral vessels is likely to be due to the activation of a PLC-coupled receptor abundantly or selectively expressed in vascular smooth muscle cells. The identification of this putative receptor could facilitate the development of tissue-selective pharmacological agents.
诺伯胺:一种对大鼠外周动脉有选择性血管收缩活性的钙通道阻滞剂。
诺伯胺是一种独特的血管活性物质,具有物种和组织特异性,内皮独立,血管收缩活性,仅限于大鼠外周动脉。在大鼠主动脉和所有其他物种的被试动脉中,诺伯胺显示血管松弛特性,可能是由于阻断钙通道。诺伯胺在离体豚鼠灌注心脏中也有钙进入阻滞作用。在这些制剂中,去甲硼胺产生冠状动脉血管扩张剂,以及负性肌力和促兴奋作用。在豚鼠单心室肌细胞中,去甲硼胺降低l型钙电流。诺伯胺选择性血管收缩作用的机制尚不清楚。在大鼠尾动脉中,该药物激活磷脂酶C (PLC)信号级联,这是大多数受体激活性血管活性药物引发收缩效应的生化途径。因此,诺伯胺诱导的大鼠周围血管收缩可能是由于在血管平滑肌细胞中大量或选择性表达的plc偶联受体的激活。该受体的鉴定有助于组织选择性药物的开发。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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