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克罗卡林对钾预收缩的兔、猫和大鼠离体脑动脉舒张作用的比较。

Comparison of cromakalim-induced relaxation of potassium precontracted rabbit, cat, and rat isolated cerebral arteries.

作者信息

Parsons A A, Ksoll E, Mackert J R, Schilling L, Wahl M

机构信息

Physiologisches Institut, Universität München, Federal Republic of Germany.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1991 Apr;343(4):384-92. doi: 10.1007/BF00179043.

Abstract

The effects of cromakalim were investigated in KCl-precontracted cat, rabbit, and rat isolated cerebral arteries with intact endothelium. Potassium induced contraction of all cerebral arteries studied, but exhibited marked vessel and species variation with no spasm to 20 or 30 mmol/l KCl in the rat basilar artery or 20 mmol/l KCl in the rabbit middle cerebral artery. On sustained tension to 20 mmol/l KCl, cromakalim induced concentration-related relaxation in the rabbit basilar artery and the cat basilar and middle cerebral arteries with Hill coefficients greater than unity. Cromakalim was more potent in the rabbit basilar artery precontracted with 20 or 30 mmol/KCl than in the rabbit middle cerebral artery or the cat basilar or middle cerebral artery. Elevation of the KCl concentration to 50 mmol/l inhibited cromakalim-induced relaxation and produced a decrease in the Hill coefficient. Preincubation of cerebral arteries with glibenclamide (100 nmol/l-1 mumol/l) produced concentration-related inhibition of the cromakalim-induced relaxation in the rabbit basilar, cat basilar, and cat middle cerebral arteries precontracted with 20 mmol/l KCl. The degree of rightward shift of concentration-effect curves by glibenclamide was calculated at the EC25, EC50, and EC75 levels. A good correlation was observed between the shifts at the EC50 and EC75 levels. However, the shift in concentration-effect curves for cromakalim produced at the EC25 level was markedly less than the EC50 or EC75 levels in the presence of 1 mumol/l glibenclamide. The pA2 values for glibenclamide calculated at the EC50 level were 6.6 +/- 0.09, 7.1 +/- 0.1, and 6.5 +/- 0.5 in the rabbit basilar, cat basilar, and cat middle cerebral artery, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在具有完整内皮的氯化钾预收缩猫、兔和大鼠离体脑动脉中研究了克罗卡林的作用。钾离子可使所有研究的脑动脉收缩,但表现出明显的血管和物种差异,大鼠基底动脉对20或30 mmol/L氯化钾以及兔大脑中动脉对20 mmol/L氯化钾无痉挛反应。在持续张力为20 mmol/L氯化钾时,克罗卡林可使兔基底动脉以及猫基底动脉和大脑中动脉产生浓度依赖性舒张,希尔系数大于1。与兔大脑中动脉或猫基底动脉及大脑中动脉相比,克罗卡林对用20或30 mmol/L氯化钾预收缩的兔基底动脉作用更强。将氯化钾浓度提高到50 mmol/L可抑制克罗卡林诱导的舒张,并使希尔系数降低。用格列本脲(100 nmol/L - 1 μmol/L)预孵育脑动脉,可对用20 mmol/L氯化钾预收缩的兔基底动脉、猫基底动脉和猫大脑中动脉产生浓度依赖性抑制克罗卡林诱导的舒张作用。在EC25、EC50和EC75水平计算格列本脲对浓度 - 效应曲线的右移程度。在EC50和EC75水平的右移之间观察到良好的相关性。然而,在存在1 μmol/L格列本脲的情况下,EC25水平时克罗卡林浓度 - 效应曲线的右移明显小于EC50或EC75水平。在兔基底动脉、猫基底动脉和猫大脑中动脉中,在EC50水平计算的格列本脲的pA2值分别为6.6±0.09、7.1±0.1和6.5±0.5。(摘要截短于250字)

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