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前列腺素H1类似物的生物活性。

Biological activities of prostaglandin H1 analogs.

作者信息

Morita A, Nishino H, Mori M, Hasegawa K, Sakai K, Kobayashi S

出版信息

Prostaglandins. 1979 Oct;18(4):529-40. doi: 10.1016/0090-6980(79)90021-2.

Abstract

The influences of epoxymethano and epoxycarbonyl analogs of PGH1 on washed rabbit platelets, isolated smooth muscles and perfused heart preparations were investigated. On washed rabbit platelets, 11,9-epoxymethano and 11,9-epoxycarbonyl PGH1 produced a platelet aggregation whereas 9,11-epoxymethano and 9,11-epoxycarbonyl PGH1 produced an inhibition of arachidonic acid-induced platelet aggregation. On iso-ated rabbit thoracic aorta strips, 9,11-epoxycarbonyl PGH1 showed strong contracting activity (5 times as active as 11,9-epoxymethano PGH2 and 31 times as active as PGH2). All the analogs of PGH1 caused contraction of guinea pig tracheal muscle and caused an increase of perfusion pressure in guinea pig heart, though 11,9-epoxymethano and epoxycarbonyl PGH1 were far more active than 9,11-epoxymethano and epoxycarbonyl PGH1. Differences in biological activities between 11,9-epoxymethano and epoxycarbonyl PGH1 indicate that the orientation of functional groups at C9 and C11 influences biological activities.

摘要

研究了PGH1的环氧甲撑和环氧羰基类似物对洗涤过的兔血小板、分离的平滑肌和灌注心脏制剂的影响。在洗涤过的兔血小板上,11,9-环氧甲撑和11,9-环氧羰基PGH1可引起血小板聚集,而9,11-环氧甲撑和9,11-环氧羰基PGH1则可抑制花生四烯酸诱导的血小板聚集。在分离的兔胸主动脉条上,9,11-环氧羰基PGH1表现出强烈的收缩活性(活性是11,9-环氧甲撑PGH2的5倍,是PGH2的31倍)。所有PGH1类似物均可引起豚鼠气管肌肉收缩,并使豚鼠心脏灌注压升高,不过11,9-环氧甲撑和环氧羰基PGH1的活性远比9,11-环氧甲撑和环氧羰基PGH1高。11,9-环氧甲撑和环氧羰基PGH1之间生物活性的差异表明,C9和C11处官能团的取向会影响生物活性。

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