陆荣发, 邹冈. 雄性抗生育剂α-氯丙二醇及其衍生物的实验药理研究J. 药学学报, 1979, 14(7): 402-407.
引用本文: 陆荣发, 邹冈. 雄性抗生育剂α-氯丙二醇及其衍生物的实验药理研究J. 药学学报, 1979, 14(7): 402-407.
Lu Rongfa, Zou gang. EXPERIMENTAL PHARMACOLOGIC STUDIES ON THE MALE ANTIFERTILITY AGENT α-CHLOROHYDRIN AND ITS ANALOGUESJ. Acta Pharmaceutica Sinica, 1979, 14(7): 402-407.
Citation: Lu Rongfa, Zou gang. EXPERIMENTAL PHARMACOLOGIC STUDIES ON THE MALE ANTIFERTILITY AGENT α-CHLOROHYDRIN AND ITS ANALOGUESJ. Acta Pharmaceutica Sinica, 1979, 14(7): 402-407.

雄性抗生育剂α-氯丙二醇及其衍生物的实验药理研究

EXPERIMENTAL PHARMACOLOGIC STUDIES ON THE MALE ANTIFERTILITY AGENT α-CHLOROHYDRIN AND ITS ANALOGUES

  • 摘要: 本文介绍α-氯丙二醇及其衍生物的药理实验结果。雄性大白鼠口服α-氯丙二醇5mg/kg/天,4天后其生育力消失。连续灌胃22~25周对雄鼠的生长发育,性行为和体内主要脏器均无明显影响,停药后生育力可恢复。大白鼠和狗灌胃22~25mg/kg/天的急性和亚急性毒性反应主要表现为肝脏细胞和小脑组织出现轻微病变,其余无异常。α-氯丙二醇产生抗生育作用主要是使雌性大白鼠输卵管中受精卵在早期发育分裂阶段发生变性退化,造成受精卵早期死亡。α-氯丙二醇使雄鼠产生不孕性交配行为,从而引起雌鼠出现假孕。我们利用这种现象,改进了蜕膜瘤模型的实验方法。此外,还筛选了35个α-氯丙二醇衍生物,工作有待继续以发现抗生育作用更佳的化合物。

     

    Abstract: The results of pharmacologic experiments on α-chlorohydrin and its analogues are reported in this paper. A prominent antifertility action of α-chlorohydrin has been demonstrated in male rats after a daily oral dose of 5 mg/kg for 5 days. Prologned medication up to 22~25 weeks did not affect the growth curves, sexual behavior, and structures of several important organs. Normal fertility recovered after cessation of the medication. Subacute toxicity tests on male rats and dogs with daily oral dose of 20~25 mg/kg revealed minor pathologic changes in liver cells and cerebellar elements.In our study, α-chlorohydrin probably exerted its antifertility action through mutagenic effect on the sperms, since fertilized ova with signs of early degeneration have been repeatedly found in the Fallopian tubes, indicating the sperms still retained their fertilizing ability.The pseudopregnancy in female rats having non-fertile mating with α-chlorohydrintreated males provided us an ideal model for reproductive physiological studies, these female rats were easily picked up by vaginal, smears, the pseudopregnancy induced being more physiologic than by other means. We have taken advantage of this model in performing deciduoma and egg transfer experiments with unexpected high rate of success.A series of 35 analogues of ’α-chlorohydrin have been screened, further work is still in progress in order to find compounds superior to the parent substance.

     

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