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[氟化前列腺素对血小板聚集的影响]

[The effect of fluorinated prostaglandins on platelet aggregation].

作者信息

Lakin K M, Makarov V A, Kovalev S G, Petrukhina G N, Serkov I V, Golovanova N K, Bezuglov V V

出版信息

Eksp Klin Farmakol. 1994 Mar-Apr;57(2):39-41.

PMID:8205047
Abstract

The effects of fluorodeoxy prostanoids on platelet aggregability were studied. It was shown that introduction of fluorine into positions 9, 11 or 15 of prostaglandin F2 alpha led to enhanced proaggregation activity. The most active compound among fluorodeoxy analogs was 15-fluoro derivative; bisfluoro analog was moderately active, and 11-fluoro compound had the least activity. In the group of fluorodeoxy prostaglandins E2, a contrary effect was registered. Thus, the most active compound was 1-fluoride and the least, 15-fluoride. The incorporation of fluorine into position 15 of prostacyclin led to insignificantly lower antiaggregatory activity just as this modification of 6-keto-prostaglandin F1 alpha was accompanied by a dramatic increase in its ability to inhibit platelet aggregation.

摘要

研究了氟脱氧前列腺素对血小板聚集性的影响。结果表明,在前列腺素F2α的9、11或15位引入氟会导致促聚集活性增强。氟脱氧类似物中活性最高的化合物是15-氟衍生物;双氟类似物活性中等,而11-氟化合物活性最低。在氟脱氧前列腺素E2组中,观察到相反的效果。因此,活性最高的化合物是1-氟化物,活性最低的是15-氟化物。将氟引入前列环素的15位会导致抗聚集活性略有降低,同样,6-酮-前列腺素F1α的这种修饰伴随着其抑制血小板聚集能力的显著增加。

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