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抗蠕虫药伊维菌素对寄生线虫猪蛔虫咽肌的作用。

Actions of the anthelmintic ivermectin on the pharyngeal muscle of the parasitic nematode, Ascaris suum.

作者信息

Brownlee D J, Holden-Dye L, Walker R J

机构信息

Division of Cell Sciences, School of Biological Sciences, University of Southampton, UK.

出版信息

Parasitology. 1997 Nov;115 ( Pt 5):553-61. doi: 10.1017/s0031182097001601.

Abstract

The anthelmintic invermectin has a number of effects on nematodes which result in changes in behaviour, particularly locomotion, including paralysis and an inhibition of feeding. This paper describes the application of an in vitro pharmacological approach to further delineate the action of ivermectin on feeding behaviour. Contraction of Ascaris suum pharyngeal muscle was monitored using a modified pressure transducer system which detects changes in intrapharyngeal pressure and therefore contraction of the radial muscle of the pharynx. The pharynx did not contract spontaneously. However, serotonin (5-HT, 100 microM) stimulated rhythmic contractions and relaxations (pumping) at a frequency of 0.5 Hz. gamma-Aminobutyric acid (GABA) and glutamic acid inhibited the pumping elicited by 5-HT. The duration of inhibition was concentration dependent (1-1000 microM) with a threshold of 1 microM and 10 microM respectively (n = 8). Ivermectin also inhibited pharyngeal pumping (1-1000 nM). At lower concentrations, ivermectin (1-10 pM) potentiated the GABA and glutamate inhibition, so that inhibition occurred at concentrations which were below threshold in the absence of ivermectin. These data provide evidence that the pharynx is a site for the action of ivermectin. Thus interruption of pharyngeal processes such as, feeding, regulation of hydrostatic pressure and secretion may provide a new site of anthelmintic action.

摘要

抗寄生虫药伊维菌素对线虫有多种作用,会导致行为改变,尤其是运动方面,包括麻痹和摄食抑制。本文描述了一种体外药理学方法的应用,以进一步阐明伊维菌素对摄食行为的作用。使用改良的压力传感器系统监测猪蛔虫咽肌的收缩情况,该系统可检测咽内压力变化,从而检测咽径向肌的收缩。咽不会自发收缩。然而,血清素(5-羟色胺,100微摩尔)以0.5赫兹的频率刺激节律性收缩和舒张(抽吸)。γ-氨基丁酸(GABA)和谷氨酸抑制5-羟色胺引起的抽吸。抑制持续时间呈浓度依赖性(1-1000微摩尔),阈值分别为1微摩尔和10微摩尔(n = 8)。伊维菌素也抑制咽抽吸(1-1000纳摩尔)。在较低浓度下,伊维菌素(1-10皮摩尔)增强了GABA和谷氨酸的抑制作用,因此在没有伊维菌素时低于阈值的浓度下就会发生抑制。这些数据证明咽是伊维菌素的作用部位。因此,诸如摄食、静水压力调节和分泌等咽过程的中断可能提供了一个新的驱虫作用位点。

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