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克罗卡林、RP49356、二氮嗪、格列本脲和甘丙肽对大鼠门静脉的作用。

Effects of cromakalim, RP49356, diazoxide, glibenclamide and galanin in rat portal vein.

作者信息

Longmore J, Newgreen D T, Weston A H

机构信息

Department of Physiological Sciences, University of Manchester, U.K.

出版信息

Eur J Pharmacol. 1990 Nov 6;190(1-2):75-84. doi: 10.1016/0014-2999(90)94114-d.

DOI:10.1016/0014-2999(90)94114-d
PMID:1706274
Abstract

The study investigated the possible involvement of an ATP-sensitive potassium (K) channel in the relaxant actions of K channel openers in rat portal vein. The effects of glibenclamide on the relaxant responses and rises in 86Rb efflux evoked by cromakalim, RP49356 and diazoxide were studied. The effects of galanin and depletion of intracellular ATP concentrations [( ATP]i) were also examined. Galanin increased mechanical activity and 86Rb efflux, effects most likely mediated via galanin receptors rather than a direct action on a K channel. Glibenclamide inhibited the relaxant responses and rises in 86Rb efflux evoked by cromakalim, RP49356 and diazoxide. Reduction of [ATP]i caused relaxation and this effect was partially reversed by glibenclamide. The restored activity was abolished by cromakalim. These results suggest that an ATP-sensitive K channel is present on rat portal vein and that it may be involved in the relaxant actions of cromakalim, RP49356 and diazoxide.

摘要

该研究调查了ATP敏感性钾(K)通道在大鼠门静脉中钾通道开放剂舒张作用中的可能参与情况。研究了格列本脲对由克罗卡林、RP49356和二氮嗪引起的舒张反应及86Rb外流增加的影响。还检测了甘丙肽的作用以及细胞内ATP浓度([ATP]i)的降低情况。甘丙肽增加了机械活性和86Rb外流,其作用很可能是通过甘丙肽受体介导的,而非直接作用于钾通道。格列本脲抑制了由克罗卡林、RP49356和二氮嗪引起的舒张反应及86Rb外流增加。[ATP]i的降低导致舒张,且这种作用被格列本脲部分逆转。恢复的活性被克罗卡林消除。这些结果表明大鼠门静脉存在ATP敏感性钾通道,且它可能参与了克罗卡林、RP49356和二氮嗪的舒张作用。

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引用本文的文献

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The effects of (-)-cromakalim and glibenclamide on uptake2 in guinea-pig trachealis muscle.(-)-克罗卡林和格列本脲对豚鼠气管平滑肌摄取2的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1993 Jul;348(1):65-9. doi: 10.1007/BF00168538.
2
Comparison of the cromakalim antagonism and bradycardic actions of a series of novel alinidine analogues in the rat.一系列新型阿利尼定类似物在大鼠体内的克罗卡林拮抗作用和心动过缓作用的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1994 Aug;350(2):158-66. doi: 10.1007/BF00241091.
3
The contribution of Rb-permeable potassium channels to the relaxant and membrane hyperpolarizing actions of cromakalim, RP49356 and diazoxide in bovine tracheal smooth muscle.
Rb 通透钾通道对克罗卡林、RP49356 和二氮嗪在牛气管平滑肌中的舒张和膜超极化作用的贡献。
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4
Comparison of the effects of several potassium-channel openers on rat bladder and rat portal vein in vitro.几种钾通道开放剂对大鼠膀胱和大鼠门静脉的体外作用比较。
Br J Pharmacol. 1991 Mar;102(3):679-86. doi: 10.1111/j.1476-5381.1991.tb12233.x.