文章基本信息

标题：AGGREGATION OF PLATELETS INDUCED BY NOVEL SYNTHETIC SECOPROSTAGLANDINS
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作者：AKIRA OHTSU ; TOSHIO TANAKA ; FUKUYOSHI KAMIMOTO 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1981
卷号：4
期号：10
页码：771-778
DOI：10.1248/bpb1978.4.771
出版社：The Pharmaceutical Society of Japan
摘要：Two series of 8-acetyl-12-hydroxyalkadienoic acids and 14-hydroxy-9-oxoalkadienoic acids which can be regarded as 11, 12-and 8, 12-secoprostaglandin E₂ were synthesized and evaluated for their biological properties. Key members of each series, 11, 12-(8Ac-HAD) and 8, 12-seco-11-norprostaglandin E₂ (14H-OAD), were found to induce platelet aggregation which were inhibited by preincubation of platelet rich plasma with prostaglandin I₂ but not inhibited by indomethacin. 8Ac-HAD produced dose-dependent potent contraction of rabbit aorta. Injection of 8Ac-HAD (1 mg/kg) into vein of rat induced sudden death of the animal. Both compounds were stable and platelet aggregating activity did not decrease at least for four hours at 0°C. Structure-activity relationship study of the series were carried out. Reduction of the acetyl carbonyl and methoxime formation of 8Ac-HAD lowered platelet aggregating acrivity, and 8-propionyl substituent and 12-deoxy derivative of 8Ac-HAD showed no activity. 12 (R)-Isomer and dl 12-methyl derivative of 8Ac-HAD retained the platelet aggregating activity. Modification of ω-chain did not cause any essential effect on the activity. Unlike 8Ac-HAD, several modification of 14H-OAD failed to maintain the aggregating activity.
关键词：fatty acid