Willcockson W S, Hillman G R
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(1):199-203. doi: 10.1016/0742-8413(84)90151-8.
Several vertebrate 5-HT antagonists at concentrations around 0.1 mM reduced 5-HT-induced increases in the motor activity of the parasitic blood fluke Schistosoma mansoni. The order of potency for 5-HT response antagonism was haloperidol greater than cyproheptadine greater than mianserin greater than trazodone greater than spiperone greater than methysergide. Nisoxetine, a 5-HT uptake inhibitor in vertebrate preparations, was also a potent antagonist of the 5-HT response in schistosomes. The potent antischistosomal praziquantel reduced the 5-HT response similarly to the other antiserotonergic drugs, but at much lower concentrations, beginning around 0.1 microM. The 5-HT agonist quipazine stimulated worm activity at 1-0.1 mM when applied alone, but reduced the 1 mM 5-HT response when quipazine and 5-HT were administered concurrently. Dopamine (DA) alone had no effect on the overall activity of S. mansoni. Although no drug was found to have absolute species specificity, quantitative differences were observed between the relative activity of drugs in schistosomes and vertebrates.
几种脊椎动物5-羟色胺（5-HT）拮抗剂在浓度约为0.1 mM时，可降低5-HT诱导的寄生血吸虫曼氏血吸虫运动活性的增加。5-HT反应拮抗效力的顺序为：氟哌啶醇大于赛庚啶大于米安色林大于曲唑酮大于螺哌隆大于甲基麦角新碱。在脊椎动物制剂中作为5-HT摄取抑制剂的尼索西汀，也是血吸虫中5-HT反应的有效拮抗剂。强效抗血吸虫药物吡喹酮与其他抗5-羟色胺能药物类似地降低了5-HT反应，但浓度要低得多，约从0.1 microM开始。5-HT激动剂喹哌嗪单独应用时在1 - 0.1 mM可刺激虫体活性，但当喹哌嗪和5-HT同时给药时可降低1 mM 5-HT的反应。多巴胺（DA）单独对曼氏血吸虫的整体活性无影响。虽然未发现有药物具有绝对的物种特异性，但观察到药物在血吸虫和脊椎动物中的相对活性存在定量差异。
