Tomlinson G, Albuquerque C A, Woods R A
Eur J Pharmacol. 1985 Jul 17;113(2):255-62. doi: 10.1016/0014-2999(85)90743-5.
The paralyzing effects of the anthelmintic drugs amidantel (BAY d 8815) and its deacylated derivative (BAY d 9216) on whole and cut C. elegans were investigated. The minimum effective concentrations with whole worms were 350 and 180 microM, respectively, compared to only 4 microM for another anthelmintic drug, levamisole. After rendering the worms permeable by cutting them at their approximate midsections, the minimum effective concentrations were: amidantel 0.30 microM, deacylated amidantel 0.07 microM and levamisole 0.15 microM. Comparison of the effects produced by amidantel and deacylated amidantel with those produced by levamisole, a known cholinergic agonist, suggested a common mode of action for all three drugs. The drugs were moderately potent inhibitors of both E. electricus and C. elegans acetylcholinesterase but at concentrations too high to account for their abilities to contract cut worms. Their primary mode of action appears to be as agonists at the level of the acetylcholine receptor, a view supported by the observation that their effects may be blocked by the nicotinic antagonists d-tubocurarine and gallamine.
研究了驱虫药氨苯达唑（BAY d 8815）及其脱酰基衍生物（BAY d 9216）对完整和切断的秀丽隐杆线虫的麻痹作用。对于完整的线虫，其最小有效浓度分别为350和180微摩尔，而另一种驱虫药左旋咪唑仅为4微摩尔。在通过在大约虫体中部切断使其可渗透后，最小有效浓度为：氨苯达唑0.30微摩尔、脱酰基氨苯达唑0.07微摩尔和左旋咪唑0.15微摩尔。将氨苯达唑和脱酰基氨苯达唑产生的效应与已知胆碱能激动剂左旋咪唑产生的效应进行比较，表明这三种药物具有共同的作用模式。这些药物是电鳐和秀丽隐杆线虫乙酰胆碱酯酶的中度有效抑制剂，但浓度过高，无法解释它们使切断的线虫收缩的能力。它们的主要作用模式似乎是作为乙酰胆碱受体水平的激动剂，这一观点得到了以下观察结果的支持：它们的效应可能被烟碱拮抗剂d -筒箭毒碱和加拉明阻断。
