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桂利嗪和氟桂利嗪,豚鼠过敏性休克的强效抑制剂。

Cinnarizine and flunarizine, potent inhibitors of anaphylactic shock in guinea-pigs.

作者信息

Awouters F, Niemegers C J, Janssen P A

出版信息

Arch Int Pharmacodyn Ther. 1975 Sep;217(1):38-43.

PMID:242287
Abstract

Histamine-induced paw oedema and anaphylactic shock were studied simultaneously in ovalbumin-sensitized guinea-pigs and cinnarizine and flunarizine were evaluated quantitatively with regard to protection from the two types of challenge. Both compounds were markedly more active in preventing lethal anaphylaxis (ED50's of 0.67 and 0.53 mg/kg OR) than in reducing histamine oedema (ED50's of 2.77 and 1.54 mg/kg OR). The high anti-anaphylactic potency after oral administration may be an important finding in view of the therapeutic applications of cinnarizine and flunarizine.

摘要

在卵清蛋白致敏的豚鼠中同时研究了组胺诱导的爪肿胀和过敏性休克,并对桂利嗪和氟桂利嗪在预防这两种激发类型方面进行了定量评估。两种化合物在预防致死性过敏反应方面(半数有效剂量分别为0.67和0.53毫克/千克口服)比减轻组胺性肿胀方面(半数有效剂量分别为2.77和1.54毫克/千克口服)明显更有效。鉴于桂利嗪和氟桂利嗪的治疗应用,口服给药后高抗过敏性效力可能是一个重要发现。

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