【摘要】 感染小鼠一次口服~3H-吡喹酮100mg/kg后,其体内两性血吸虫的~3H含量以给药后0.5～1小时为最高,4小时后则有明显减少。体外培养的血吸虫亦能迅速摄取~3H-吡喹酮,且其摄入量随药物浓度的增加而递增。体内、体外试验的结果表明,最初进入虫体的~3H-吡喹酮系脂溶性,随后在体内缓慢代谢为水溶性。放射自显影的结果说明,~3H主要自表皮进入虫体,分布于肌层、间充组织、生殖系统和肠壁上皮细胞,其中以雌虫的卵黄腺为最多,而以雄虫的睾丸为最少。更多还原

【Abstract】 Within 0.5～1 hour after administration of ~3H-pyquiton to mice infected with Schistosoma japonicum at a single dose of 100 mg/kg, the radioactivity levels of the worms reached maximum, but declined markedly 4 hours later In vitro, the uptake of ~3H-pyquiton by bisexual worms maintained in cultural medium was also prompt. Moreover, the radioactivity levels of the worms increased with the concentrations of the drug.It was demonstrated that the labelled pyquiton absorbed initially by the schistosome was fat-soluble, and was metabolized gradually in the worms and transformed into water-soluble metabolites.Autoradiography showed that ~3H-pyquiton entered into worms by simple diffusion mechanism and distributed in musculature, parenchyma, reproductive system and epithelial cells of the intestine. Maximum radioactivity was observed in the vitelline gland of female worm, and minimum in the testes of male schistosomes.更多还原