Some biological effects of prostaglandin endoperoxide analogs.

Some biological effects of prostaglandin endoperoxide analogs.
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前列腺素内过氧化物类似物的一些生物效应。

DOI:
10.1016/0024-3205(76)90021-7
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发表时间:
1976
期刊:
影响因子:
6.1
通讯作者:
C. Malmsten
C. Malmsten
中科院分区:
医学2区
文献类型:
--
作者:
C. Malmsten

文献摘要

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前列腺素内过氧化物 PGG2 和 PGH2 的两种甲氧基类似物的作用在人血小板和兔主动脉条上进行了测试。其中一种类似物 9α, 11α-methano-epoxy-15- Hydroxy-prosta-5, 13-dienoic Acid 作为聚集剂,其引发离体兔主动脉收缩的活性比内过氧化物 PGG2 强 3.7 倍,并且比 PGH2 强 6.2 倍。该类似物引发血小板释放反应,但在这方面不如内过氧化物活跃。此外,由该类似物诱导的 14 C-血清素的释放被吲哚美辛抑制,这表明需要产生内过氧化物。在所采用的测试系统中,相应的9α,11α,环氧-甲氧基-类似物的活性低于9α,11α,甲氧基-环氧类似物。
The effects of two methano-epoxy analogs of the prostaglandin endoperoxides PGG2and PGH2were tested on human platelets and rabbit aorta strips. One of these analogs, 9α, 11α-methano-epoxy-15- hydroxy-prosta-5, 13-dienoic acid, was 3.7 times more potent than the endoperoxide, PGG2, as aggregating agent and was 6.2 times more active than PGH2in eliciting contractions of the isolated rabbit aorta. The analog initiated the platelet release reaction, but was less active than the endoperoxide in this respect. Furthermore, the release of14C-serotonin induced by this analog was inhibited by indomethacin, which indicated that generation of endoperoxide was required.The corresponding 9α, 11α, epoxy-methano-analog was less active than the 9α, 11α, methano-epoxy analog in the test systems employed.