Fairweather I, Holmes S D, Threadgold L T
Exp Parasitol. 1984 Jun;57(3):209-24. doi: 10.1016/0014-4894(84)90094-8.
The effects of a wide range of fasciolicides on the in vitro motility of Fasciola hepatica have been determined by means of an isometric transducer system. Carbon tetrachloride and diamphenethide do not affect movement at concentrations up to 500 and 100 micrograms/ml, respectively; at 1000 micrograms/ml, however, carbon tetrachloride induces a rapid tonic paralysis. Brotianide and the deacetylated metabolite of diamphenethide cause a rapid flaccid paralysis of the fluke at concentrations of 1.0 micrograms/ml and above. In contrast, the effect of MK-401 is a long-term one, a flaccid paralysis occurring after 20 hr only at 200 micrograms/ml. Praziquantel also produces a flaccid paralysis of the fluke, but this follows an initial increase, then decrease in muscle tone. The effect is rapid at 500 micrograms/ml, but long-term at 100 and 200 micrograms/ml; at these lower concentrations there is also a stimulation of activity. Oxyclozanide , rafoxanide, niclofolan , bithionol, and hexacholorophene induce a rapid spastic paralysis of the fluke at concentrations of 1.0 micrograms/ml and above. Both phasic and tonic components are evident in the response at concentrations of 1.0 micrograms/ml and below; the phasic component disappears at higher concentrations. Nitroxynil produces a similar effect, evident at higher concentrations. Among the benzimidazoles, mebendazole, oxfendazole, and albendazole sulphoxide cause a suppression of motility, whilst thiabendazole and albendazole produce a stimulation of movement. The effects are not rapid, however, for only mebendazole at 500 micrograms/ml causes total inactivity of the fluke within a 12-hr period. Possible explanations for these effects on fluke motility are discussed.
利用等长换能器系统测定了多种杀片形吸虫药对肝片形吸虫体外运动能力的影响。四氯化碳和双胺苯噻唑分别在浓度高达500微克/毫升和100微克/毫升时不影响虫体运动；然而，在1000微克/毫升时，四氯化碳会引起迅速的强直性麻痹。溴替尼和双胺苯噻唑的脱乙酰代谢产物在浓度为1.0微克/毫升及以上时会使吸虫迅速发生弛缓性麻痹。相比之下，MK - 401的作用是长期的，仅在200微克/毫升时20小时后才会出现弛缓性麻痹。吡喹酮也会使吸虫发生弛缓性麻痹，但这是在肌肉张力先升高后降低之后出现的。在500微克/毫升时作用迅速，但在100和200微克/毫升时作用是长期的；在这些较低浓度下也会刺激虫体活动。羟氯扎胺、雷复尼特、硝氯酚、硫双二氯酚和六氯酚在浓度为1.0微克/毫升及以上时会引起吸虫迅速的痉挛性麻痹。在1.0微克/毫升及以下浓度时，反应中的相性和强直性成分都很明显；在较高浓度时相性成分消失。硝碘酚腈产生类似的效果，在较高浓度时明显。在苯并咪唑类药物中，甲苯咪唑、奥芬达唑和阿苯达唑亚砜会抑制虫体运动，而噻苯达唑和阿苯达唑会刺激虫体运动。然而，这些作用并不迅速，因为只有500微克/毫升的甲苯咪唑会在12小时内使吸虫完全失去活动能力。文中讨论了这些对吸虫运动能力影响的可能解释。
