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米安色林与可乐定在α2-肾上腺素能受体上的相互作用。

Interaction between mianserin and clonidine at alpha 2-adrenoceptors.

作者信息

Pommier Y, Andréjak M, Mouillé P, Dabiré H, Lucet B, Schmitt H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):288-94. doi: 10.1007/BF00501167.

Abstract

The purpose of the present study was to characterize the effects of mianserin at alpha 2-adrenoceptors. Firstly, the action of mianserin on postganglionic sympathetic fibres has been studied using the tachycardia induced by stimulation of the cardiac nerve in dogs. Mianserin increased this tachycardia, but could not prevent the inhibitory effect of clonidine in this model. However, an antagonistic effect of mianserin against clonidine was observed when animals were pretreated with desipramine. Secondly, mianserin antagonized the inhibitory effect of clonidine on the electrically stimulated guinea-pig ileum. In high concentrations, mianserin reduced both electrically and acetylcholine induced contractions. Thirdly, mianserin antagonised the sleep induced by clonidine in chickens. These results are consistent with alpha 2-adrenoceptor blocking properties of mianserin in peripheral noradrenergic fibres in dogs, in cholinergic fibres in guinea-pig ileum and in the central nervous system in chickens.

摘要

本研究的目的是表征米安色林对α2-肾上腺素能受体的作用。首先,利用刺激犬心神经诱发的心动过速,研究了米安色林对节后交感神经纤维的作用。米安色林使这种心动过速加剧,但在该模型中不能阻止可乐定的抑制作用。然而,当动物用去甲丙咪嗪预处理时,观察到米安色林对可乐定有拮抗作用。其次,米安色林拮抗可乐定对电刺激的豚鼠回肠的抑制作用。在高浓度时,米安色林减少电刺激和乙酰胆碱诱导的收缩。第三,米安色林拮抗可乐定在鸡中诱导的睡眠。这些结果与米安色林在犬外周去甲肾上腺素能纤维、豚鼠回肠胆碱能纤维和鸡中枢神经系统中的α2-肾上腺素能受体阻断特性一致。

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