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拉贝洛尔对离体灌注大鼠肠系膜中肾上腺素能受体的作用。

Effect of labetalol on adrenoceptors in the isolated perfused rat mesentery.

作者信息

Gulati N, Huggel H, Gulati O P

出版信息

Arch Int Pharmacodyn Ther. 1980 Aug;246(2):251-6.

PMID:7436629
Abstract

Isolated perfused rat mesentery has been used to define alpha- and beta-adrenoceptors. Norepinephrine was used as a reference substance to induce vasoconstrictor responses (increase in perfusion pressure). Log-dose response curves were obtained in the dose range between 0.3-10 mug. Labetalol, a known competitive inhibitor of both alpha- and beta-adrenoceptors, when administered as a single bolus injection (3 mug) initially induced predominant alpha-blockade lasting upto 75 min followed by potentiation of the vasoconstrictor responses to norepinephrine used at multiple dose levels. This potentiation was maximum between 150-195 min after injection of labetalol. This potentiating effect of labetalol observed in the later phase of the experiment might be related to its inhibitory mechanism of neuronal uptake.

摘要

离体灌注大鼠肠系膜已被用于确定α和β肾上腺素能受体。去甲肾上腺素被用作参考物质以诱导血管收缩反应(灌注压力升高)。在0.3 - 10微克的剂量范围内获得了对数剂量反应曲线。拉贝洛尔是一种已知的α和β肾上腺素能受体的竞争性抑制剂,当作为单次推注注射(3微克)时,最初会引起持续长达75分钟的主要α阻断,随后在多个剂量水平下增强对去甲肾上腺素的血管收缩反应。这种增强作用在注射拉贝洛尔后150 - 195分钟之间最大。在实验后期观察到的拉贝洛尔的这种增强作用可能与其对神经元摄取的抑制机制有关。

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