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[利血平对α受体阻滞剂效能的影响]

[Effect of reserpine on the potency of alpha receptor blockers].

作者信息

Benthe V H, Göthert M, Krug J

出版信息

Arzneimittelforschung. 1975 Mar;25(3):402-7.

PMID:239728
Abstract

The influence of rather low doses of reserpine (0.125--2.0 mg/kg) on the pressor effect of noradrenaline (NA) was studied in pithed rats. In addition it was investigated whether the blocking activity of alpha-sympathicolytic agents is influenced by pretreatment with reserpine. 24 h after injection of these doses of reserpine this drug only increased the pressor effect of lower doses of NA without shifting the dose-response curve to the left. As a rule in rats pretreated with reserpine the affinity of alpha-blocking agents (derivatives of phenylethylamine and phenoxyethylamine) to alpha-adrenoceptors is not considerably altered. Only two phenylethylamine derivates substituted with a p-hydroxy group possessed considerably higher blocking activity in reserpine pretreated animals than in rats not pretreated. The increase in sensitivity of blood vessels against low doses of NA (250 pg and 1 ng) observed in rats pretreated with reserpine is abolished even by alpha-blocking substances with low affinity to alpha-adrenoceptors.

摘要

在脊髓横断的大鼠中研究了相当低剂量的利血平(0.125 - 2.0毫克/千克)对去甲肾上腺素(NA)升压作用的影响。此外,还研究了α-交感神经阻滞剂的阻断活性是否受利血平预处理的影响。注射这些剂量的利血平24小时后,该药物仅增强了较低剂量NA的升压作用,而未使剂量反应曲线向左移动。通常,在用利血平预处理的大鼠中,α-阻滞剂(苯乙胺和苯氧乙胺衍生物)对α-肾上腺素受体的亲和力没有明显改变。只有两种对羟基取代的苯乙胺衍生物在利血平预处理的动物中比未预处理的大鼠具有明显更高的阻断活性。即使是对α-肾上腺素受体亲和力低的α-阻断物质,也能消除在用利血平预处理的大鼠中观察到的血管对低剂量NA(250皮克和1纳克)敏感性的增加。

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