全钰珠, 黄婉芸, 周歧新, 李远宗. 4-硝基二苯胺-4'-硫代氨基甲酸(O)苯酯的抗血吸虫作用及毒性J. 药学学报, 1982, 17(7): 481-486.
引用本文: 全钰珠, 黄婉芸, 周歧新, 李远宗. 4-硝基二苯胺-4'-硫代氨基甲酸(O)苯酯的抗血吸虫作用及毒性J. 药学学报, 1982, 17(7): 481-486.
QUAN Yu-zhu, HUANG Wan-yun, ZHOU Qi-xin , LI Yuan-zong, . STUDIES ON THE ANTISCHISTOSOMAL ACTION AND TOXICITY OF PHENYL 4-NITRO-DIPHENYLAMINO 4'-THIONCARBAMATE (7720)J. Acta Pharmaceutica Sinica, 1982, 17(7): 481-486.
Citation: QUAN Yu-zhu, HUANG Wan-yun, ZHOU Qi-xin , LI Yuan-zong, . STUDIES ON THE ANTISCHISTOSOMAL ACTION AND TOXICITY OF PHENYL 4-NITRO-DIPHENYLAMINO 4'-THIONCARBAMATE (7720)J. Acta Pharmaceutica Sinica, 1982, 17(7): 481-486.

4-硝基二苯胺-4'-硫代氨基甲酸(O)苯酯的抗血吸虫作用及毒性

STUDIES ON THE ANTISCHISTOSOMAL ACTION AND TOXICITY OF PHENYL 4-NITRO-DIPHENYLAMINO 4'-THIONCARBAMATE (7720)

  • 摘要: 本文证明硝硫氰胺(C 9333-(Go/CGP 4540)类的衍生物4-硝基二苯胺-4′-硫代氨基甲酸(O)苯酯(代号7720)有与硝硫氰胺同等强度的抗血吸虫作用。用粗粉混悬液灌胃治疗小白鼠实验性血吸虫病,7720和硝硫氰胺的CD50分别为79.0μmol/kg/d(即28.8mg/kg/d)×5日和83.4μmol/kg/d(即22.6mg/kg/d)×5日。7720 16或32 mg/kg/d×5d已可使所试全部病免达寄生虫学治愈。未能测出小白鼠灌胃急性LD50。通过对幼年大白鼠体重增长影响的观察,家犬亚急性毒性试验及内脏组织病理学检查等提示本药经口给药无严重毒性反应。本文还证明4-硝基-4′-异硫氰基二苯醚对家兔实验性血吸虫病亦有较佳疗效。

     

    Abstract: The antischistosomal action and toxicity of phenyl-4-nitrodiphenylamino-4'-thioncarbamate (7720), a new compound related to Amoscanate (C9333-Go/CGP4540),were studied. The results of our experiments showed that 7720 exhibited a dramatic curative effect as C9333 on experimental schistosomiasis. The 50% curative dose (CD50) of 7720 and C9333 given intragastrically in mice against S. japonicum was 79.0 μmol/kg/day (or 28.8 mg/kg/day)×5 and 83.4 μmol/kg/day (or 22.6 mg/kg/day)×5, respectively. The rabbits infected with S. japonicum were free from worms of both sexes after treatment with 7720 by dosage regimes of either 16 or 32 mg/kg/day for 5 consecutive days. 7720 was tolerated asymptomatically by mice in a single oral dose of 5 g/kg. The results obtained by the oral subacute toxicity test on dogs and rats, including observation of the effect on the body weight growth rate of young rats, liver function and renal function tests, hematological routine test, EKG as well as histopathological examination showed that 7720 displayed few toxic actions. The therapeutic effect of Lopatol, a diphenyl ether analogue of C9333, was also studied in rabbits infected with S. japonicum. All the rabbits treated with Lopatol were completely cured by a dosage regime of 40 mg/kg/day×5, intragastrically.

     

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