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可乐定、胍法辛和B-HT 920对大鼠多种炎症原诱导的急性爪肿胀的抗炎作用。

Anti-inflammatory actions of clonidine, guanfacine and B-HT 920 against various inflammagen-induced acute paw oedema in rats.

作者信息

Kulkarni S K, Mehta A K, Kunchandy J

出版信息

Arch Int Pharmacodyn Ther. 1986 Feb;279(2):324-34.

PMID:3516094
Abstract

Clonidine (0.1-1.0 mg/kg, i.p.) exhibited anti-inflammatory activity in carrageenan-, formalin-, 5-HT- and histamine-induced paw oedema in rats. Similarly, other two alpha 2-adrenoceptor agonists, guanfacine and B-HT 920, also displayed an anti-inflammatory action in these models. The anti-inflammatory effect of all the three alpha 2-adrenoceptor agonists was reversed by yohimbine. However, prazosin failed to block the anti-inflammatory effect of clonidine. Intracerebroventricularly administered clonidine had a delayed onset of anti-inflammatory action, starting only from 60 min post carrageenan administration. This was in contrast to the systemically administered clonidine which was effective against both phases of carrageenan-induced oedema. On the other hand, irrespective of the route of administration, i.e. peripheral or central, guanfacine and B-HT 920 were effective against the early as well as against the delayed phases of the inflammatory reaction. The studies suggest that it is not the imidazoline moiety but the activation of alpha 2-adrenoceptors which is essential for the anti-inflammatory action of these agents.

摘要

可乐定(0.1 - 1.0毫克/千克,腹腔注射)在角叉菜胶、福尔马林、5 - 羟色胺和组胺诱导的大鼠爪肿胀模型中表现出抗炎活性。同样,另外两种α2 - 肾上腺素能受体激动剂胍法辛和B - HT 920在这些模型中也显示出抗炎作用。这三种α2 - 肾上腺素能受体激动剂的抗炎作用均被育亨宾逆转。然而,哌唑嗪未能阻断可乐定的抗炎作用。脑室内注射可乐定的抗炎作用起效延迟,仅在注射角叉菜胶60分钟后才开始。这与全身给药的可乐定不同,全身给药的可乐定对角叉菜胶诱导的肿胀的两个阶段均有效。另一方面,无论给药途径是外周还是中枢,胍法辛和B - HT 920对炎症反应的早期和延迟阶段均有效。这些研究表明,对于这些药物的抗炎作用而言,关键不是咪唑啉部分,而是α2 - 肾上腺素能受体的激活。

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