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(±)和(+)15-甲基PGF甲酯的抗早孕作用

Effects of (±) and (+) 15-Methyl PGF Methyl Ester on Early Pregnancy

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【作者】 王乃功关慕贞左晓春

【Author】 Wang Naigong; Guan Muzhen; Zuo Xiaochun(Institute of Materia Medica, CAMS and PUMC,Beijing 100050)

【机构】 中国医学科学院中国协和医科大学药物研究所!北京100050

【摘要】 15-甲基PGF2α甲酯(PG05)对小鼠有明显的抗早孕作用。(+)PGOS为有活性的立体异构体,其抗早孕和致腹泻作用均比(±)PGOS强,治疗指数与(±)PG05基本一致。大鼠于妊娠第7、8、9天,皮下注射(±)PG050.5mg/kg有明显的抗早孕作用;同样剂量的PGOS对去卵巢后,靠外源性孕酮和雌酮维持妊娠的大鼠无抗早孕作用。PGOS20μg/ml既可抑制hCG刺激黄体细胞分泌cAMP,又能桔抗SBr-cAMP刺激黄体细胞分泌孕酮,PG05可能在2个或2个以上环节上抑制大鼠卵巢黄体功能。

【Abstract】 Treatment with 15-methyl PGF,. methyl ester (PG05) resulted in termination of pregnancy and peristatic effects in mice. (+) PGO5 is the active stereoisomer of racemic PG05.The therapuetic index of (+) PG05 was found to be closely similar to that of (±) PG05.Pregnancy of ovariectomized rats given progesterone and estrone was maintained normally.PG05 was shown to have no effect on the gestation of ovariectomized rats receiving progesterone and estrone injection. PG05 at a concentration of 20μg/ml reduced cAMP secretion ofrat luteal cells in response to hCG in vitro. PG05 at concentration of 10 and 20μg/ml also exerted an inhibitory effect on 8 Br-cAMP-stimulated progesterone production. These resultssuggest that in luteal cells PG05 inhibits steroidogenesis at the steps of gonadotropin-stimulated cAMP formation and cAMP-induced progesterone production.

  • 【文献出处】 中国医学科学院学报 ,Acta Academiae Medicinae Sinicae , 编辑部邮箱 ,1994年03期
  • 【分类号】R169.42;R9
  • 【被引频次】4
  • 【下载频次】19
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