{"title":"地拉西普的新衍生物K-7259对腺苷心血管作用的影响:与地拉西普的比较。","authors":"A Hara, M Akahira, Y Abiko","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>The effect of K-7259, a novel derivative of dilazep, on the cardiovascular action of adenosine was studied in the aortic ring and isolated perfused heart in guinea-pigs, and compared with that of dilazep. Adenosine produced a concentration-dependent relaxation in phenylephrine (2 x 10(-6) M)-contracted aortic rings and exhibited a negative chronotropic effect in the isolated perfused heart. Dilazep (10(-8), 10(-7) and 10(-6) M) potentiated significantly the relaxing action of adenosine on the aortic ring in a concentration-dependent way. K-7259 (10(-6) M), however, did not potentiate the relaxing action of adenosine, although the high concentration of K-7259 (10(-5) M) potentiated it slightly but significantly. The negative chronotropic effect of adenosine was also potentiated by dilazep (10(-7) and 10(-6) M), but not by K-7259 (10(-6) M). These results suggest that the potentiating action of K-7259 on the cardiovascular effects of adenosine is very weak when compared with that of dilazep.</p>","PeriodicalId":8166,"journal":{"name":"Archives internationales de pharmacodynamie et de therapie","volume":"330 1","pages":"66-75"},"PeriodicalIF":0.0000,"publicationDate":"1995-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Effect of K-7259, a novel derivative of dilazep, on cardiovascular actions of adenosine: comparison with dilazep.\",\"authors\":\"A Hara, M Akahira, Y Abiko\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The effect of K-7259, a novel derivative of dilazep, on the cardiovascular action of adenosine was studied in the aortic ring and isolated perfused heart in guinea-pigs, and compared with that of dilazep. Adenosine produced a concentration-dependent relaxation in phenylephrine (2 x 10(-6) M)-contracted aortic rings and exhibited a negative chronotropic effect in the isolated perfused heart. Dilazep (10(-8), 10(-7) and 10(-6) M) potentiated significantly the relaxing action of adenosine on the aortic ring in a concentration-dependent way. K-7259 (10(-6) M), however, did not potentiate the relaxing action of adenosine, although the high concentration of K-7259 (10(-5) M) potentiated it slightly but significantly. The negative chronotropic effect of adenosine was also potentiated by dilazep (10(-7) and 10(-6) M), but not by K-7259 (10(-6) M). These results suggest that the potentiating action of K-7259 on the cardiovascular effects of adenosine is very weak when compared with that of dilazep.</p>\",\"PeriodicalId\":8166,\"journal\":{\"name\":\"Archives internationales de pharmacodynamie et de therapie\",\"volume\":\"330 1\",\"pages\":\"66-75\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-07-01\",\"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}
Effect of K-7259, a novel derivative of dilazep, on cardiovascular actions of adenosine: comparison with dilazep.
The effect of K-7259, a novel derivative of dilazep, on the cardiovascular action of adenosine was studied in the aortic ring and isolated perfused heart in guinea-pigs, and compared with that of dilazep. Adenosine produced a concentration-dependent relaxation in phenylephrine (2 x 10(-6) M)-contracted aortic rings and exhibited a negative chronotropic effect in the isolated perfused heart. Dilazep (10(-8), 10(-7) and 10(-6) M) potentiated significantly the relaxing action of adenosine on the aortic ring in a concentration-dependent way. K-7259 (10(-6) M), however, did not potentiate the relaxing action of adenosine, although the high concentration of K-7259 (10(-5) M) potentiated it slightly but significantly. The negative chronotropic effect of adenosine was also potentiated by dilazep (10(-7) and 10(-6) M), but not by K-7259 (10(-6) M). These results suggest that the potentiating action of K-7259 on the cardiovascular effects of adenosine is very weak when compared with that of dilazep.