{"title":"trapidil及其衍生物对花生四烯酸注射大鼠血栓素A2产生的抑制作用","authors":"Ingrid Heinroth-Hoffmann, A. Hauser, H.-J. Mest","doi":"10.1016/0262-1746(87)90138-7","DOIUrl":null,"url":null,"abstract":"<div><p>Trapidil and four selected 5,7-disubstituted s-triazolo (1,5-a)pyrimidine derivatives (AR 12456, AR 12463, AR 12464, AR 12465) which have already been shown to possess inhibitory effects on arachidonic acid(AA)-induced aggregation and thromboxane A<sub>2</sub>(TXA<sub>2</sub>) formation in human and rabbit platelets in vitro diminished the AA-stimulated TXAZ production in murine blood in vivo. The inhibitory effects of the derivatives were generally stronger than those of trapidil. The strongest inhibitor of TXA<sub>2</sub> formation was the derivative AR 12456. These in vivo results correspond well with our previous in vitro findings.</p></div>","PeriodicalId":20720,"journal":{"name":"Prostaglandins, leukotrienes, and medicine","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1987-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0262-1746(87)90138-7","citationCount":"14","resultStr":"{\"title\":\"Inhibition of thromboxane A2 production by trapidil and trapidil derivatives in the arachidonic acid-injected rat\",\"authors\":\"Ingrid Heinroth-Hoffmann, A. Hauser, H.-J. Mest\",\"doi\":\"10.1016/0262-1746(87)90138-7\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Trapidil and four selected 5,7-disubstituted s-triazolo (1,5-a)pyrimidine derivatives (AR 12456, AR 12463, AR 12464, AR 12465) which have already been shown to possess inhibitory effects on arachidonic acid(AA)-induced aggregation and thromboxane A<sub>2</sub>(TXA<sub>2</sub>) formation in human and rabbit platelets in vitro diminished the AA-stimulated TXAZ production in murine blood in vivo. The inhibitory effects of the derivatives were generally stronger than those of trapidil. The strongest inhibitor of TXA<sub>2</sub> formation was the derivative AR 12456. These in vivo results correspond well with our previous in vitro findings.</p></div>\",\"PeriodicalId\":20720,\"journal\":{\"name\":\"Prostaglandins, leukotrienes, and medicine\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1987-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0262-1746(87)90138-7\",\"citationCount\":\"14\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Prostaglandins, leukotrienes, and medicine\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/0262174687901387\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Prostaglandins, leukotrienes, and medicine","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0262174687901387","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 14
摘要
Trapidil和四种选定的5,7-二取代s-三唑(1,5-a)嘧啶衍生物(AR 12456, AR 12463, AR 12464, AR 12465)已经被证明在体外对人和兔血小板中花生四烯酸(AA)诱导的聚集和血栓素A2(TXA2)的形成具有抑制作用，在体内可以减少AA刺激的小鼠血液中TXAZ的产生。这些衍生物的抑制作用普遍强于trapidil。最强的TXA2形成抑制剂是衍生物AR 12456。这些体内结果与我们之前的体外研究结果吻合得很好。
Inhibition of thromboxane A2 production by trapidil and trapidil derivatives in the arachidonic acid-injected rat
Trapidil and four selected 5,7-disubstituted s-triazolo (1,5-a)pyrimidine derivatives (AR 12456, AR 12463, AR 12464, AR 12465) which have already been shown to possess inhibitory effects on arachidonic acid(AA)-induced aggregation and thromboxane A2(TXA2) formation in human and rabbit platelets in vitro diminished the AA-stimulated TXAZ production in murine blood in vivo. The inhibitory effects of the derivatives were generally stronger than those of trapidil. The strongest inhibitor of TXA2 formation was the derivative AR 12456. These in vivo results correspond well with our previous in vitro findings.
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