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二氢吡啶PN 202 - 791的激动剂和拮抗剂对映体作用于血管平滑肌电压依赖性钙通道不同位点的证据。

Evidence that agonist and antagonist enantiomers of the dihydropyridine PN 202-791 act at different sites on the voltage-dependent calcium channel of vascular muscle.

作者信息

Hughes A D, Hering S, Bolton T B

机构信息

Department of Pharmacology and Clinical Pharmacology, St. George's Hospital Medical School, London.

出版信息

Br J Pharmacol. 1990 Sep;101(1):3-5. doi: 10.1111/j.1476-5381.1990.tb12076.x.

DOI:10.1111/j.1476-5381.1990.tb12076.x
PMID:2282463
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1917649/
Abstract

S(+)-PN 202-791, a calcium channel agonist, and its optical isomer R(-)-PN 202-791, a calcium channel antagonist, respectively increased and decreased inward current carried by barium through voltage-dependent calcium channels in isolated ear artery cells of the rabbit in a concentration-dependent manner. The EC50 or IC50 derived from the concentration-response relationship was unaltered in the presence of the other enantiomer indicating that no competitive antagonism exists between these enantiomers and suggesting that the actions of these two enantiomers involve two separate binding sites.

摘要

S(+)-PN 202-791是一种钙通道激动剂，其旋光异构体R(-)-PN 202-791是一种钙通道拮抗剂，它们分别以浓度依赖性方式增加和减少了钡通过家兔离体耳动脉细胞中电压依赖性钙通道所携带的内向电流。从浓度-反应关系得出的EC50或IC50在另一种对映体存在时未发生改变，这表明这些对映体之间不存在竞争性拮抗作用，并提示这两种对映体的作用涉及两个不同的结合位点。

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本文引用的文献

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Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches.用于从细胞和无细胞膜片进行高分辨率电流记录的改进膜片钳技术。
Pflugers Arch. 1981 Aug;391(2):85-100. doi: 10.1007/BF00656997.
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1,4-Dihydropyridine activators and antagonists: structural and functional distinctions.1,4 - 二氢吡啶激活剂与拮抗剂：结构与功能差异
Trends Pharmacol Sci. 1989 Dec;10(12):507-11. doi: 10.1016/0165-6147(89)90051-5.
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Calcium currents in single isolated smooth muscle cells from the rabbit ear artery in normal-calcium and high-barium solutions.正常钙溶液和高钡溶液中兔耳动脉单个分离平滑肌细胞的钙电流。
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Nonmodal gating of cardiac calcium channels as revealed by dihydropyridines.二氢吡啶揭示的心脏钙通道非模式门控
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5
Voltage- and use-dependent modulation of cardiac calcium channels by the dihydropyridine (+)-202-791.二氢吡啶（+）-202-791对心脏钙通道的电压依赖性和使用依赖性调节
Circ Res. 1989 Feb;64(2):338-51. doi: 10.1161/01.res.64.2.338.
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