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舒洛芬,一种对大鼠醋酸诱导扭体反应有强效拮抗作用的物质。

Suprofen, a potent antagonist of acetic acid-induced writhing in rats.

作者信息

Niemegeers C J, Van Bruggen J A, Janssen P A

出版信息

Arzneimittelforschung. 1975 Oct;25(10):1505-9.

PMID:1243029
Abstract

A new standardized acetic acid-induced writhing test in rats is described in detail and its methodology is discussed briefly. The described method has proved to be useful for evaluating the anti-writhing activity of narcotic analgesics, non-narcotic anti-inflammatory compounds and narcotic-antagonists with analgesic activity. A direct quantitative comparison of anti-writhing activity was made between orally administered acetyl-salicylic acid, phenylbutazone, indometacin, tolmetin, ketoprofen and alpha-methyl-4-(2-thienylcarbonyl)benzeneacetic acid (suprofen) in a specially designed experiment. Among the known non-narcotic, non-steroidal anti-inflammatory compounds suprofen appeared to be the most potent antagonist of acetic acid-induced writhing in rats, about 200 to 300 times as potent as acetyl-salicylic acid and phenylbutazone, 15 to 30 times as potent as indometacin and tolmetin, and about 6 times as potent as ketoprofen.

摘要

本文详细描述了一种新的标准化大鼠醋酸诱导扭体试验,并简要讨论了其方法。所描述的方法已被证明可用于评估麻醉性镇痛药、非麻醉性抗炎化合物和具有镇痛活性的麻醉拮抗剂的抗扭体活性。在一项专门设计的实验中,对口服乙酰水杨酸、保泰松、吲哚美辛、托美丁、酮洛芬和α-甲基-4-(2-噻吩羰基)苯乙酸(舒洛芬)的抗扭体活性进行了直接定量比较。在已知的非麻醉性、非甾体抗炎化合物中,舒洛芬似乎是大鼠醋酸诱导扭体最有效的拮抗剂,其效力约为乙酰水杨酸和保泰松的200至300倍,吲哚美辛和托美丁的15至30倍,酮洛芬的约6倍。

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