EFFECT OF PRAZIQUANTEL DERIVATIVE S83143 AND ITS SALTS ON INFECTION OF SCHISTOSOMA JAPONICUM IN MICE
- VernacularTitle:吡喹酮衍生物S83143及其盐类对小鼠血吸虫的杀灭作用
- Author:
Wenju YUE
;
Jingyan MEI
- Publication Type:Journal Article
- Keywords:
Praziquantel;
Derivative of praziquantel;
Schistosoma japonicum;
Schistosomula
- From:
Chinese Pharmacological Bulletin
1987;0(02):-
- CountryChina
- Language:Chinese
-
Abstract:
Effect of S83143, a praziquantel derivative, and its phosphate salt S85009, sulfate salt S85010 and hydrochloride salt S85021 on different developmental stages of Schistosoma japonicum in mice were ob- served. When infected mice were treated with S83143 suspension at a single oral dose of 400 mg/kg or with 3 different salts of S83143 at a single intramuscular dose of 100 mg' ( S83143 base )/kg, the worm reduction rate was 69~87% in 2 h old schistosomula and 47~96% in 32~33 d old adult worms, respectively, but had no effect on 3 ~14 d schistosomula. The results showed that the susceptibility of different developmental stages of schistosome to S83143 was similar to that of praziquantel.The acute LD50 of ig S83143 suspension was more than 10g/kg, while ED50 was 352?65 mg/kg. With im S85010 solution, the LD50 and ED50 were 176?14 and 66?10 mg/kg respectively. Therefore, the therapeutic index of S83143 was over 28, which was higher than 2.67 of S8S010.
