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抗流感化合物的相对效价。

The relative potencies of anti-influenza compounds.

作者信息

Tisdale M, Bauer D J

出版信息

Ann N Y Acad Sci. 1977 Mar 4;284:254-63. doi: 10.1111/j.1749-6632.1977.tb21958.x.

Abstract

The relative potencies of some standard anti-influenza compounds have been examined in vitro by plaque reduction in calf kidney cells, and in vivo by reduction in virus titers of the lungs of infected mice. Strains belonging to the four subtypes H0N1, H1N1, H2N2, and H3N2 were employed to compare the activity of amantadine hydrochloride and ribavirin. In vitro for all strains except A/NWS/OO(H0N1) amantadine hydrochloride was 3-4 times more active than ribavirin. In vivo with sensitive strains amantadine hydrochloride produced a plateau effect at higher dose levels, but at lower dose levels was marginally more active than ribavirin. The sensitivity of A/Hong Kong/1/68 (H3N2) to amantadine hydrochloride, rimantadine hydrochloride, cyclooctylamine, and ribavirin was also investigated. In vitro rimantadine hydrochloride was similar in activity to amantadine hydrochloride and ribavirin, but cyclooctylamine was considerably less active. In vivo cyclooctylamine was active only at 150 mg/kg/day, whereas rimantadine hydrochloride produced a plateau effect over a range of concentrations from 9,12-150 mg/kg/day.

摘要

已通过在小牛肾细胞中进行蚀斑减少试验在体外检测了一些标准抗流感化合物的相对效价,并通过降低感染小鼠肺部的病毒滴度在体内进行了检测。使用属于H0N1、H1N1、H2N2和H3N2四种亚型的毒株来比较盐酸金刚烷胺和利巴韦林的活性。在体外,除了A/NWS/OO(H0N1)之外,对于所有毒株,盐酸金刚烷胺的活性比利巴韦林高3至4倍。在体内,对于敏感毒株,盐酸金刚烷胺在较高剂量水平时产生平台效应,但在较低剂量水平时其活性略高于利巴韦林。还研究了A/香港/1/68(H3N2)对盐酸金刚烷胺、盐酸金刚乙胺、环辛胺和利巴韦林的敏感性。在体外,盐酸金刚乙胺的活性与盐酸金刚烷胺和利巴韦林相似,但环辛胺的活性则低得多。在体内,环辛胺仅在150mg/kg/天时具有活性,而盐酸金刚乙胺在9.12至150mg/kg/天的浓度范围内产生平台效应。

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