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二氢吡啶BAY-K-8644可激活嗜铬细胞钙通道。

Dihydropyridine BAY-K-8644 activates chromaffin cell calcium channels.

作者信息

García A G, Sala F, Reig J A, Viniegra S, Frías J, Fontériz R, Gandía L

出版信息

Nature. 1984;309(5963):69-71. doi: 10.1038/309069a0.

Abstract

Douglas and Rubin suggested that "the role of acetylcholine as a transmitter at the adrenal medulla is to cause some brief change in medullary cells which allows Ca ions to penetrate them and trigger the catecholamine ejection process". The Ca2+-channel blocking agents, verapamil, nifedipine and nitrendipine, have been used widely to investigate the properties of slow Ca2+ channels in a variety of tissues, including the adrenomedullary chromaffin cell. Recently, small modifications to the nifedipine molecule produced a derivative, BAY-K-8644 (methyl-1,4-dihydro-2, 6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)-pyridine-5-carboxylate), that in contrast to the Ca2+-channel blocking agents, stimulated cardiac and vascular smooth muscle contractility. We have tested whether this compound behaves as a Ca2+-channel activator at the chromaffin cell membrane as shown by Schramm et al. in smooth muscle cells. The experiments described here strongly suggest that it does so.

摘要

道格拉斯和鲁宾提出,“乙酰胆碱作为肾上腺髓质递质的作用是使髓质细胞发生一些短暂变化,从而使钙离子能够穿透细胞并触发儿茶酚胺释放过程”。钙通道阻滞剂维拉帕米、硝苯地平和尼群地平已被广泛用于研究包括肾上腺髓质嗜铬细胞在内的多种组织中慢钙通道的特性。最近,对硝苯地平分子进行了微小修饰,得到了一种衍生物BAY-K-8644(1,4-二氢-2,6-二甲基-3-硝基-4-(2-三氟甲基苯基)-吡啶-5-羧酸甲酯),与钙通道阻滞剂相反,它能刺激心脏和血管平滑肌收缩。我们已经测试了这种化合物在嗜铬细胞膜上是否像施拉姆等人在平滑肌细胞中所表明的那样作为钙通道激活剂起作用。这里描述的实验有力地表明它确实如此。

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