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一类新型抗溃疡药物。I. 4-苯基-四氢异喹啉衍生物AN5对大鼠不同溃疡实验模型的抗溃疡作用。

A new class of antiulcer drugs. I. Antiulcer effect of AN5, a 4-phenyl-tetrahydroisoquinoline derivative, on different experimental models of ulcer in rats.

作者信息

Ivanova N, Mondeshka D, Ivanov C, Angelova I, Terziyska S, Paskov V

机构信息

Research and Development Department, Chemical Pharmaceutical Works, Sofia, Bulgaria.

出版信息

Methods Find Exp Clin Pharmacol. 1990 Jul-Aug;12(6):401-10.

PMID:2087139
Abstract

The action of AN5 on experimental models of gastric ulcers induced by water-immersion stress, indomethacin and reserpine, or by pylorus ligation in rats has been studied. AN5 supresses the formation of ulcers in all experimental models. The strongest antiulcer effect is shown in relation to water-immersion stress-induced ulcers. From the broad pharmacological studies of AN5 on this model it can be seen that even a dose of 0.100 mg/kg has a high antiulcer activity. The increase of the dose leads to a regular increase of the antiulcer activity, the highest suppression of the ulcer index being reached at a dose of 1 mg/kg (86.15%). The comparative studies with ranitidine and cimetidine on the same experimental models of gastric ulcers show that AN5 possesses an antiulcer activity many times higher than that of the above-mentioned drugs.

摘要

研究了AN5对大鼠水浸应激、消炎痛和利血平或幽门结扎诱导的胃溃疡实验模型的作用。AN5在所有实验模型中均能抑制溃疡的形成。对水浸应激诱导的溃疡显示出最强的抗溃疡作用。从对该模型进行的广泛药理学研究可以看出,即使剂量为0.100mg/kg也具有很高的抗溃疡活性。剂量增加会导致抗溃疡活性有规律地增加,在剂量为1mg/kg时溃疡指数的抑制率最高(86.15%)。在相同的胃溃疡实验模型上与雷尼替丁和西咪替丁进行的比较研究表明,AN5具有比上述药物高许多倍的抗溃疡活性。

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