Terada M, Sano M
Z Parasitenkd. 1986;72(3):375-85. doi: 10.1007/BF00928748.
Effects of piperazine derivatives, especially of diethylcarbamazine (DEC) on adult Angiostrongylus cantonensis and Dirofilaria immitis were examined. Piperazine (3 X 10(-5)-10(-4) M) paralyzed A. cantonensis and the action was antagonized by picrotoxin. 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP) (10(-5)-10(-4) M) caused contraction but little effect was produced by strychnine. An inhibitory effect on untreated preparations was caused by lower concentrations (3 X 10(-6)-10(-5) M) of diethylcarbamazine citrate (DEC) and also on the preparations contracted by eserine. A stimulatory effect was also seen when higher concentrations (10(-4)-3 X 10(-4) M) of this drug were applied to both preparations. The inhibitory action of DEC was antagonized by gabergic antagonists such as picrotoxin and bicuculline, but not by alpha-adrenergic antagonists like dibenamine and phentolamine. When the worm preparation was paralyzed by strychnine or hexylresorcinol (inhibitors of the release of acetylcholine in this worm), the stimulatory effect of DEC was blocked, but pyrantel (a nicotinic cholinergic agonist) contracted the paralyzed preparation. However, the effect of DEC on D. immitis (10(-7)-3 X 10(-4) M) was inhibitory, and this action was also antagonized by picrotoxin. These results suggest that the DEC inhibitory and stimulatory action is through the gabergic and cholinergic mechanisms in adult A. cantonensis and D. immitis.
研究了哌嗪衍生物，尤其是枸橼酸乙胺嗪（DEC）对成年广州管圆线虫和犬恶丝虫的作用。哌嗪（3×10⁻⁵ - 10⁻⁴ M）可使广州管圆线虫麻痹，且该作用可被印防己毒素拮抗。碘化1,1 - 二甲基 - 4 - 苯基哌嗪（DMPP）（10⁻⁵ - 10⁻⁴ M）可引起收缩，但士的宁对此作用影响较小。较低浓度（3×10⁻⁶ - 10⁻⁵ M）的枸橼酸乙胺嗪（DEC）对未处理的标本以及被毒扁豆碱收缩的标本均有抑制作用。当将该药物的较高浓度（10⁻⁴ - 3×10⁻⁴ M）应用于这两种标本时，也可观察到刺激作用。DEC的抑制作用可被γ - 氨基丁酸能拮抗剂如印防己毒素和荷包牡丹碱拮抗，但不能被α - 肾上腺素能拮抗剂如双苄胺和酚妥拉明拮抗。当虫体标本被士的宁或己基间苯二酚（该虫体中乙酰胆碱释放的抑制剂）麻痹时，DEC的刺激作用被阻断，但噻嘧啶（一种烟碱型胆碱能激动剂）可使麻痹的标本收缩。然而，DEC对犬恶丝虫（10⁻⁷ - 3×10⁻⁴ M）的作用是抑制性的，且该作用也可被印防己毒素拮抗。这些结果表明，DEC的抑制和刺激作用是通过成年广州管圆线虫和犬恶丝虫中的γ - 氨基丁酸能和胆碱能机制实现的。
