摘要
三氟乙酰伯氨喹(M 8506)对小鼠、大鼠与犬的毒性明显低于伯氨喹(PQ)。小鼠 igM 8506的LD50为 PQ 的3倍。大鼠 igM 8506 30mg/(kg·d)×28d,犬 ig 2mg/(kg·d)×28d 无不良反应。犬 ig量≥5mg/(kg·d)时有消化道反应,肝、肾与心等受损。6只犬 igM 8506 10mg/(kg·d),3只犬完成21d疗程;2只犬 ig 同剂量 PQ 1～2剂后均死亡。M 8506无诱变性。
5-Trifluoroacetylprimaquine(M8506),which has higher radicalcurative effect against Plasmodium cynomolgi than primaquine(PQ),was found tobe less toxic in mice,rats and house dogs than PQ.The acute LD50 of oralM8506 in mice was 263～278 mg/kg,at least 3 times as that of PQ(61～69 mg/kg).The M8506 doses in rats 30 mg/(kg·d)×28d and in dogs 2 mg/(kg·d)×28dwere free from any side effects.When dogs received≥5 mg/(kg·d)of M8506,toxic reactions in gastrointestinal tract,increase of salivary and ophthalmic secre-tion,and deteriorative hepatic and renal functions were observed.At the samedose of 10 mg/(kg·d),3 of 6 dogs finished a 21d course of M8506 therapy,whileboth dogs receiving PQ died after 1 or 2 doses.The results of Ames test,chromosomal aberration test and mouse micronu-cleus test were all negative.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1991年第4期164-166,177,共4页
Chinese Journal of Pharmaceuticals
关键词
抗疟药
伯氨喹
毒性
诱变性
antimalarials
8-aminoquinolines
primaquine
5-trifluoroacetylprimapuine
toxicity
mutagenicity
