发现一种可逆的男性避孕药剂来源于隆尼达胺
Shengnan Gong1, Shiyao Zhu1, Peng Zhou1
1Institute of Reproductive Medicine, School of Medicine, Nantong University, Nantong, Jiangsu 226019, P. R. China.
ACS omega
|May 30, 2023
概括
一种新的非荷尔蒙男性避孕药 (BHD) 在一次剂量后在小鼠中显示出100%的有效性. 这种可逆的药物破坏了精子细胞的产生和血液丸屏障,为男性避孕开发提供了一个有前途的候选人.
科学领域:
- 生殖生物学 生殖生物学
- 药理学 药理学是指药理学的学科.
- 药物发现 药物发现
背景情况:
- 与女性选择相比,男性非激素避孕药的需求很高,但研究不足.
- 现有的候选药物,如龙尼达胺和阿朱丁,面临着阻碍发展的毒性挑战.
- 需要一种新的方法来创造安全有效的男性避孕药.
研究的目的:
- 设计和合成由隆尼达胺衍生的新型非荷尔蒙男性避孕药.
- 评估新药 (BHD) 在雄性动物中的避孕疗效和可逆性.
- 阐明BHD对精子生成和血液丸屏障的作用机制.
主要方法:
- 基于结构连接体的设计被用来合成新的分子.
- 在雄性小鼠和大鼠中通过口服BHD.的服用来测试避孕疗效.
- 分析了精子生成细胞的亡和血液丸屏障的破坏.
主要成果:
- 一种新型化合物BHD在两周一次性口服剂量 (100或500毫克/体重) 后,在雄性小鼠中显示出100%的避孕疗效. ) 的情况.
- 在治疗后6周观察到生育能力下降 (BHD-100的90%和BHD-500的50%).
- BHD迅速诱导了精子生成细胞的亡,并有效地破坏了血液丸屏障.
结论:
- BHD是一种强效的,可逆的,非激素的男性避孕药.
- 它的机制涉及诱导精子细胞的亡,并危及血屏障.
- BHD代表了未来男性避孕药开发的有希望的候选人.
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