可乐定的抗溃疡活性:对胃前列腺素缺乏作用

Prostaglandins, leukotrienes, and medicine Pub Date : 1987-11-01 DOI:10.1016/0262-1746(87)90024-2

Z. Ben-Zvi, V. Leibson

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引用次数: 3

摘要

可乐定和对氨基可乐定对消炎痛引起的雌性大鼠胃溃疡的形成有抑制作用。这种保护作用被联合施用育亨宾阻断。因此，可乐定的抗溃疡活性是由于其外周α -2的激动作用。由于吲哚美辛是一种前列腺素合成酶抑制剂，其致溃疡作用归因于前列腺素(PG)缺乏的状态。因此，我们研究了α -2肾上腺素能受体激动剂的保护作用可能是通过刺激胃中PGs的生物合成来介导的。然而，无论是否使用吲哚美辛，结果均未显示体外胃片或可乐定预处理大鼠胃粘膜中PGE2或6-酮- pgf1的产生增加。由此可见，可乐定对消炎痛所致大鼠胃糜烂的预防作用可能与前列腺素无关。

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Antiulcer activity of clonidine: lack of effect on gastric prostaglandins

Clonidine and paraaminoclonidine prevented the formation of indomethacin-induced gastric ulcers in female rats. This protective activity was blocked by coadministration of yohimbine. Therefore, the antiulcer activity of clonidine was due to its peripheral alpha-2 agonistic action. Because indomethacin is a prostaglandin synthetase inhibitor, its ulcerogenic effect has been attributed to a state of prostaglandin (PG) deficiency. We therefore investigated the possibility that the protective effect of alpha-2 adrenoceptor agonists could be mediated by stimulation of the biosynthesis of PGs in the stomach. However, the results failed to show incresed production of PGE₂ or 6-keto-PGF1, either in stomach slices $in vitro$ or in the gastric mucosa of rats pretreated with clonidine, whether indomethacin was used or not. It is concluded that the activity of clonidine in preventing indomethacin-induced gastric erosions in rats is probably not related to prostaglandins.

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Prostaglandins, leukotrienes, and medicine

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