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(N-哌啶甲基)-2-色满对大鼠突触前和突触后α-肾上腺素能受体的体内和体外研究

[In vivo and in vitro study of (N-piperidinomethyl)-2-chromanne on pre- and postsynaptic alpha-adrenoreceptors in the rat].

作者信息

Mouillé P, Payard M, Henry P, Tronche P, Schmitt H

出版信息

J Pharmacol. 1985 Apr-Jun;16(2):181-9.

PMID:2997547
Abstract

The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg/kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats. On the vas deferens of the rat (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on the twitch response produced by electrical stimulation and also the contractions induced by phenylephrine. This derivate appears to be an alpha 1 and alpha 2 blocking agent.

摘要

在大鼠体内和体外研究了(N-哌啶甲基)-2-色满的α-肾上腺素能受体阻断作用。在脊髓横断大鼠中,(N-哌啶甲基)-2-色满(静脉注射1mg/kg)拮抗α激动剂诱导的升压作用。(N-哌啶甲基)-2-色满竞争性拮抗M7(α2激动剂)和可乐定(α1激动剂)的升压作用。(N-哌啶甲基)-2-色满拮抗可乐定对刺激的脊髓横断大鼠突触前α2受体的抑制作用。在大鼠输精管上,(N-哌啶甲基)-2-色满拮抗可乐定对电刺激产生的抽搐反应的抑制作用以及去氧肾上腺素诱导的收缩作用。该衍生物似乎是一种α1和α2阻断剂。

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