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奎宁和奎尼丁的非带电形式对内皮细胞容积激活氯电流的强效阻断作用。

Potent block of volume-activated chloride currents in endothelial cells by the uncharged form of quinine and quinidine.

作者信息

Voets T, Droogmans G, Nilius B

机构信息

KU Leuven, Laboratorium Voor Fysiologie, Belgium.

出版信息

Br J Pharmacol. 1996 Aug;118(7):1869-71. doi: 10.1111/j.1476-5381.1996.tb15616.x.

DOI:10.1111/j.1476-5381.1996.tb15616.x
PMID:8842456
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1909854/
Abstract
  1. The effects of quinine and quinidine on the volume-activated chloride current (ICl(vol)) in cultured endothelial cells from bovine pulmonary artery were studied by use of the whole-cell patch-clamp technique. 2. At pH 7.4 both quinine and quinidine induced a fast and reversible block of ICl(vol)) with Ki values of 20 +/- 4 microM and 30 +/- 10 microM, respectively. 3. The blocking efficiency of both drugs increased dramatically with increasing extracellular pH, indicating that the blockade is mediated by the uncharged form of quinine and quinidine. 4. These results suggest a hydrophobic interaction with high affinity between volume-activated chloride channels and uncharged quinine and quinidine within the membrane bilayer of endothelial cells.
摘要
  1. 运用全细胞膜片钳技术研究了奎宁和奎尼丁对牛肺动脉培养内皮细胞中容积激活氯电流（ICl(vol)）的影响。2. 在pH 7.4时，奎宁和奎尼丁均可快速且可逆地阻断ICl(vol)，其抑制常数（Ki）值分别为20±4微摩尔/升和30±10微摩尔/升。3. 两种药物的阻断效率均随细胞外pH升高而显著增加，表明这种阻断作用是由奎宁和奎尼丁的非带电形式介导的。4. 这些结果提示，在血管内皮细胞膜双层结构中，容积激活氯通道与非带电的奎宁和奎尼丁之间存在高亲和力的疏水相互作用。

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本文引用的文献

1
Characterization of volume-activated chloride currents in endothelial cells from bovine pulmonary artery.
J Membr Biol. 1996 Feb;149(3):189-97. doi: 10.1007/s002329900019.
2
Blockers of volume-activated Cl- currents inhibit endothelial cell proliferation.容积激活氯电流阻滞剂可抑制内皮细胞增殖。
Pflugers Arch. 1995 Nov;431(1):132-4. doi: 10.1007/BF00374387.
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Volume-activated chloride currents in pancreatic duct cells.胰腺导管细胞中的容积激活氯电流。
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Inhibition of volume-activated chloride currents in endothelial cells by chromones.色酮对内皮细胞容积激活氯电流的抑制作用。
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Volume regulation in a toad epithelial cell line: role of coactivation of K+ and Cl- channels.蟾蜍上皮细胞系中的体积调节：钾离子通道和氯离子通道共同激活的作用
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Pharmacological and physiological significance of ion channels and factors that modulate them in vascular tissues.离子通道及其在血管组织中调节因子的药理学和生理学意义。
Pharmacol Rev. 1995 Sep;47(3):387-573.
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Volume-sensitive chloride channels associated with human cervical carcinogenesis.
Cancer Res. 1995 Dec 15;55(24):6077-83.
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Volume-regulatory taurine release from a human lung cancer cell line. Evidence for amino acid transport via a volume-activated chloride channel.人肺癌细胞系中容量调节性牛磺酸释放。通过容量激活氯离子通道进行氨基酸转运的证据。
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Mechanosensitive Ca2+ transients in endothelial cells from human umbilical vein.人脐静脉内皮细胞中的机械敏感Ca2+瞬变
Proc Natl Acad Sci U S A. 1994 Apr 12;91(8):2940-4. doi: 10.1073/pnas.91.8.2940.
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Permeation properties and modulation of volume-activated Cl(-)-currents in human endothelial cells.人内皮细胞中容积激活的Cl(-)电流的渗透特性及调节
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