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5(6)-(4-甲基哌啶-1-基)羰基苯并咪唑-2-氨基甲酸甲酯在实验性蠕虫病中的驱虫谱

Anthelmintic profile of methyl 5(6)-(4-methylpiperidin-1-yl) carbonylbenzimidazole-2-carbamate in experimental helminthiases.

作者信息

Gupta S, Khan A M, Jain M K, Katiyar J C, Naim S S, Singh S K, Sharma S

机构信息

Parasitology Division, Central Drug Research Institute, Lucknow, India.

出版信息

Indian J Exp Biol. 1990 May;28(5):475-9.

PMID:2401522
Abstract

Biological evaluation of methyl 5(6)-(4-methylpiperidin-1-yl) carbonylbenzimidazole-2-carbamate against Ancylostoma ceylanicum, Nippostrongylus brasiliensis, Syphacia obvelata, Hymenolepis nana, H. diminuta and Cysticercus fasciolaris in experimental animals is reported. The compound (mg/kg) causes 100% elimination of A. ceylanicum (25 x 1), N. brasiliensis (100 x 1), S. obvelata (50 x 1), H. nana (250 x 3) and C. fasciolaris (50 x 10). It was also effective against the developing larvae (L3, L4 and L5) of A. ceylanicum at a single oral dose of 100 mg/kg. Another study indicated that the compound elicits 100% response within 32 hr of drug administration. The drug is well tolerated and LD50 is greater than 4500 mg/kg.

摘要

报告了5(6)-(4-甲基哌啶-1-基)羰基苯并咪唑-2-氨基甲酸甲酯对实验动物体内的锡兰钩口线虫、巴西日圆线虫、鼠管状线虫、微小膜壳绦虫、缩小膜壳绦虫和豆状囊尾蚴的生物学评价。该化合物(毫克/千克)能使锡兰钩口线虫(25×1)、巴西日圆线虫(100×1)、鼠管状线虫(50×1)、微小膜壳绦虫(250×3)和豆状囊尾蚴(50×10)100%被清除。以100毫克/千克的单次口服剂量给药时,它对锡兰钩口线虫的发育幼虫(L3、L4和L5)也有效。另一项研究表明,该化合物在给药后32小时内引发100%的反应。该药物耐受性良好,半数致死量大于4500毫克/千克。

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