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新型化合物HUK 978的体外组胺H2拮抗剂活性

In vitro histamine H2-antagonist activity of the novel compound HUK 978.

作者信息

Coombes J D, Norris D B, Rising T J, Ross B C, Steward A

出版信息

Life Sci. 1985 Nov 4;37(18):1711-8. doi: 10.1016/0024-3205(85)90299-1.

Abstract

Histamine stimulated adenylate cyclase from guinea-pig fundic mucosa and 3H-tiotidine binding in guinea-pig cerebral cortex were used to assess the in-vitro histamine H2-activity of the novel H2-antagonist HUK 978. The results showed that HUK 978 was a more potent H2-antagonist than either cimetidine or ranitidine. HUK 978 was also shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors.

摘要

组胺刺激豚鼠胃底黏膜的腺苷酸环化酶以及豚鼠大脑皮层中3H-替丁的结合,以此来评估新型H2拮抗剂HUK 978的体外组胺H2活性。结果显示,HUK 978是一种比西咪替丁或雷尼替丁更强效的H2拮抗剂。研究还表明,HUK 978对组胺H1受体、毒蕈碱受体以及α和β肾上腺素能受体均无活性。

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