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关于5-氧杂-17-苯基-18,19,20-三降前列环素1α甲酯及结构相关前列腺素终止猴妊娠和抑制猴黄体的进一步研究。

Additional studies on pregnancy termination and inhibition of the monkey corpus luteum with 5-oxa-17-phenyl-18,19,20-trinor-PGF1 alpha methyl ester and structurally related prostaglandins.

作者信息

Wilks J W, Nelson N A

出版信息

Prostaglandins. 1984 Sep;28(3):323-32. doi: 10.1016/0090-6980(84)90020-0.

Abstract

Oral administration of 5-oxa-17-phenyl-18,19,20-trinor-PGF1 alpha methyl ester (PGF-analog) resulted in a consistent and dose-dependent inhibition of corpus luteum progesterone production in nonpregnant rhesus monkeys concomitantly treated with human chorionic gonadotropin. Similarly, vaginal suppositories containing PGF-analog also inhibited the monkey corpus luteum. Side effects by the oral route of administration were minimal, whereas side effects following vaginal treatment with PGF-analog were higher. Five prostaglandins with structural similarity to PGF-analog were studied for their ability to inhibit the monkey corpus luteum, but none showed an advantage over the parent molecule. PGF-analog did not synergize with 9-deoxo-16,16-dimethyl-9-methylene-PGE2 for the inhibition of the monkey corpus luteum, nor did it synergize with (15S)-15-methyl-PGF2 alpha methyl ester for the interruption of early pregnancy in the monkey. 9-Deoxo-9-methylene-5-oxa-17-phenyl-18,19-20-trinor-PGE1 methyl ester did not terminate early gestation in the monkey at doses of 8 or 24 mg.

摘要

对同时接受人绒毛膜促性腺激素治疗的未怀孕恒河猴口服5-氧杂-17-苯基-18,19,20-三降-PGF1α甲酯(PGF类似物),可导致黄体孕酮生成受到持续且剂量依赖性的抑制。同样,含PGF类似物的阴道栓剂也能抑制猴黄体。口服给药的副作用极小,而PGF类似物经阴道治疗后的副作用则较多。研究了5种与PGF类似物结构相似的前列腺素抑制猴黄体的能力,但它们均未显示出比母体分子更具优势。PGF类似物与9-脱氧-16,16-二甲基-9-亚甲基-PGE2对猴黄体的抑制作用无协同效应,与(15S)-15-甲基-PGF2α甲酯对猴早期妊娠的中断作用也无协同效应。9-脱氧-9-亚甲基-5-氧杂-17-苯基-18,19-20-三降-PGE1甲酯在8毫克或24毫克剂量时未能终止猴的早期妊娠。

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