11-脱氧前列腺素E类似物（9-酮前列炔酸）对前列腺素E2诱导的大鼠垂体前叶环磷酸腺苷积累的抑制作用。

Inhibition of prostaglandin E2-induced cyclic amp accumulation in the rat anterior pituitary by 11-deoxyprostaglandin E analogs (9-ketoprostynoic acids).

作者信息

Lippmann W

出版信息

Prostaglandins. 1975 Sep;10(3):479-91. doi: 10.1016/0090-6980(75)90128-8.

Abstract

The effects of various 11-deoxyprostaglandin E analogs on the basal and prostaglandin E2 (PGE2)-induced cyclic AMP accumulation in the rat anterior pituitary were studied in vitro. 13-Hydroxy-9-oxoprost-14-ynoic acid at 5 X 10(-4)M but not 5 X 10(-5)M, decreased (45%) the induced accumulation and did not alter the basal accmulation; 15-hydroxy-9-oxoprost-13-ynoic acid at 5 X 10(-4)M caused less of a decrease (29%) in the induced and also did not alter the basal accumulation. (14Z)-13-Hydroxy-9-oxoprost-14-enoic acid at 5 X 10(-4)M did not alter the induced and caused a slight increase (5 fold) in the basal accumulation. 7-Oxa-13-prostynoic acid increased slightly the basal accumulation at 5 X 10(-5)M (2 fold) and 2.33 X 10(-4)M (6-fold) and did not antagonize the induced accumulation. Thus, the 9-ketoprostynoic acids are effective PGE2 antagonists in this system.

摘要

在体外研究了各种11-脱氧前列腺素E类似物对大鼠垂体前叶基础状态及前列腺素E2（PGE2）诱导的环磷酸腺苷（cAMP）积累的影响。5×10⁻⁴M的13-羟基-9-氧代前列腺-14-炔酸可降低（45%）诱导的cAMP积累，但5×10⁻⁵M时则无此作用，且对基础积累无影响；5×10⁻⁴M的15-羟基-9-氧代前列腺-13-炔酸对诱导的cAMP积累的降低作用较小（29%），对基础积累也无影响。5×10⁻⁴M的（14Z）-13-羟基-9-氧代前列腺-14-烯酸对诱导的cAMP积累无影响，但使基础积累略有增加（5倍）。5×10⁻⁵M（2倍）和2.33×10⁻⁴M（6倍）的7-氧杂-13-炔前列腺酸可使基础积累略有增加，且不拮抗诱导的积累。因此，在该系统中，9-酮代炔前列腺酸是有效的PGE2拮抗剂。