{"title":"吲哚咔唑和双吲哚蛋白激酶C抑制剂对兔肾动脉的体外血管松弛作用。","authors":"S Fabre, M Prudhomme","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>The effects of 12 compounds, structurally related to the indolocarbazole bacterial metabolite staurosporine, on caffeine-induced contractions in rabbit renal arteries were studied. Eight of these compounds are effective protein kinase C inhibitors, the others are inactive towards the enzyme. The results show a link between the protein kinase C inhibitory activity and the inhibition of vascular smooth muscle contraction. However, a strong inhibition of protein kinase C is required to observe the vasorelaxant effect.</p>","PeriodicalId":8166,"journal":{"name":"Archives internationales de pharmacodynamie et de therapie","volume":"329 3","pages":"397-404"},"PeriodicalIF":0.0000,"publicationDate":"1995-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"In vitro vasorelaxant effects of indolocarbazole and bis-indole protein kinase C inhibitors on rabbit renal arteries.\",\"authors\":\"S Fabre, M Prudhomme\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The effects of 12 compounds, structurally related to the indolocarbazole bacterial metabolite staurosporine, on caffeine-induced contractions in rabbit renal arteries were studied. Eight of these compounds are effective protein kinase C inhibitors, the others are inactive towards the enzyme. The results show a link between the protein kinase C inhibitory activity and the inhibition of vascular smooth muscle contraction. However, a strong inhibition of protein kinase C is required to observe the vasorelaxant effect.</p>\",\"PeriodicalId\":8166,\"journal\":{\"name\":\"Archives internationales de pharmacodynamie et de therapie\",\"volume\":\"329 3\",\"pages\":\"397-404\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Archives internationales de pharmacodynamie et de therapie\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Archives internationales de pharmacodynamie et de therapie","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
In vitro vasorelaxant effects of indolocarbazole and bis-indole protein kinase C inhibitors on rabbit renal arteries.
The effects of 12 compounds, structurally related to the indolocarbazole bacterial metabolite staurosporine, on caffeine-induced contractions in rabbit renal arteries were studied. Eight of these compounds are effective protein kinase C inhibitors, the others are inactive towards the enzyme. The results show a link between the protein kinase C inhibitory activity and the inhibition of vascular smooth muscle contraction. However, a strong inhibition of protein kinase C is required to observe the vasorelaxant effect.
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