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9-脱氧-16,16-二甲基-9-亚甲基前列地尔E2的合成及生物学特性

Synthesis and biological properties of 9-deoxo-16,16-dimethyl-9-methylene-PGE2.

作者信息

Kimball F A, Bundy G L, Robert A, Weeks J R

出版信息

Prostaglandins. 1979 May;17(5):657-66. doi: 10.1016/s0090-6980(79)80038-6.

Abstract

The in vivo monkey uterine stimulating potency of 9-deoxy-16,16-dimethyl-9-methylene-PGE2 is similar to that of 16,16-dimethyl-PGE2 and approximately 15 times that of PGE2. Low doses of this compound stimulated uterine contractions when administered vaginally. Pregnancy was terminated prematurely following subcutaneous, intramuscular or vaginal suppository treatment. Estimates of potential for gastrointestinal side effects using the rat enteropooling assay and in vivo monkey effects indicate that diarrhea will be substantially reduced with retention of uterine stimulating potency.

摘要

9-脱氧-16,16-二甲基-9-亚甲基-PGE2在体内对猴子宫的刺激效力与16,16-二甲基-PGE2相似,约为PGE2的15倍。低剂量的该化合物经阴道给药时可刺激子宫收缩。皮下、肌肉注射或阴道栓剂治疗后可使妊娠提前终止。使用大鼠肠内积液试验和对猴的体内效应评估胃肠道副作用的可能性表明,在保留子宫刺激效力的情况下,腹泻将大幅减少。

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