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以色列金蝎毒液抑制BRL 34915诱导的86Rb+从大鼠门静脉流出。

Leiurus quinquestriatus venom inhibits BRL 34915-induced 86Rb+ efflux from the rat portal vein.

作者信息

Quast U, Cook N S

机构信息

Cardiovascular Unit, Sandoz Ltd, Basle, Switzerland.

出版信息

Life Sci. 1988;42(7):805-10. doi: 10.1016/0024-3205(88)90654-6.

DOI:10.1016/0024-3205(88)90654-6
PMID:2448575
Abstract

The effect of the crude venom of the Israeli scorpion Leiurus quinquestriatus hebraeus on the 86Rb+ efflux stimulated by the K+ channel opener BRL 34915 in the rat portal vein was examined. Applied alone, the venom greatly increased the spontaneous mechanical activity of and the concomitant 86Rb+ efflux from the vessel. When the excitability of the vein was suppressed by the dihydropyridine calcium antagonist, PN 200-110, the 86Rb+ efflux stimulated by BRL 34915 could be shown to be inhibited by the venom. From the concentration dependence of this inhibition an IC50 value of 0.17 +/- 0.01 mg/ml was estimated. This venom is thus the most potent blocker of BRL 34915-evoked 86Rb+ efflux reported so far.

摘要

研究了以色列金蝎Leiurus quinquestriatus hebraeus的粗毒液对钾通道开放剂BRL 34915刺激的大鼠门静脉86Rb+外流的影响。单独应用时,毒液极大地增加了血管的自发机械活性以及随之而来的86Rb+外流。当用二氢吡啶类钙拮抗剂PN 200 - 110抑制静脉的兴奋性时,可证明毒液能抑制BRL 34915刺激的86Rb+外流。根据这种抑制的浓度依赖性,估计IC50值为0.17±0.01mg/ml。因此,这种毒液是迄今为止报道的对BRL 34915诱发的86Rb+外流最有效的阻滞剂。

相似文献

1
Leiurus quinquestriatus venom inhibits BRL 34915-induced 86Rb+ efflux from the rat portal vein.以色列金蝎毒液抑制BRL 34915诱导的86Rb+从大鼠门静脉流出。
Life Sci. 1988;42(7):805-10. doi: 10.1016/0024-3205(88)90654-6.
2
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引用本文的文献

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Smooth muscle K+ channel openers; their pharmacology and clinical potential.平滑肌钾通道开放剂;其药理学及临床应用潜力
Pflugers Arch. 1989;414 Suppl 1:S99-105. doi: 10.1007/BF00582256.
2
Effects of potassium channel toxins from Leiurus quinquestriatus hebraeus venom on responses to cromakalim in rabbit blood vessels.来自以色列金蝎毒液的钾通道毒素对兔血管中对克罗卡林反应的影响。
Br J Pharmacol. 1989 Nov;98(3):817-26. doi: 10.1111/j.1476-5381.1989.tb14610.x.
3
Pertussis toxin treatment does not inhibit the effects of the potassium channel opener BRL 34915 on rat isolated vascular and cardiac tissues.
百日咳毒素处理并不抑制钾通道开放剂BRL 34915对大鼠离体血管和心脏组织的作用。
Naunyn Schmiedebergs Arch Pharmacol. 1988 Jan;337(1):98-104. doi: 10.1007/BF00169484.
4
Action of cromakalim on potassium membrane conductance in isolated heart myocytes of frog.克罗卡林对蛙离体心肌细胞钾膜电导的作用。
Br J Pharmacol. 1990 Jul;100(3):581-7. doi: 10.1111/j.1476-5381.1990.tb15850.x.
5
Use of toxins to study potassium channels.利用毒素研究钾通道。
J Bioenerg Biomembr. 1991 Aug;23(4):615-46. doi: 10.1007/BF00785814.