作为新型抗抗药的卡尔衍生的大麻二醇反体
Rochelle M Hines1, April Contreras1, Adriana Carrillo1
1Department of Psychology, Psychological & Brain Sciences, Interdisciplinary Neuroscience Program, University of Nevada Las Vegas, Las Vegas, NV, USA.
概括
研究人员开发了新的合成大麻 (CBD) 化合物来治疗发育性. 一种带有延长基链的化合物 (+) -CBD-oct,在小鼠模型中显示有望减少发作和改善大脑发育.
科学领域:
- 神经科学和药理学 神经科学和药理学
- 的研究研究.
- 药物发现 药物发现 药物发现
背景情况:
- 发育性综合征涉及发作和发育延迟,由于副作用和折射性,目前的抗药物往往管理不善.
- 大麻素 (CBD) 是一种非精神药物植物性大麻素,具有抗发作作用,但适用性有限.
- 现有的抗药向GABA-A受体,影响发育中的大脑.
研究的目的:
- 为了确定发育性综合征的新疗法.
- 为了表征来自非大麻卡的合成CBD (+) 反体.
- 为了建立CBD同源的结构-活性关系.
主要方法:
- 合成CBD同源的基于EEG的结构-活性关系评估.
- 在野生类型和Gabra2-1小鼠发育性模型中对 (+) -CBD-oct的评估.
- 在 (+) -CBD-oct治疗后评估抗性,死亡率和树突脊柱表型.
主要成果:
- 合成CBD同源物上长长的基链会增加功效, (+) -CBD-oct会影响δ和θ频段.
- (+) -CBD-oct预治疗增强了野生型和Gabra2-1小鼠的抗性和降低了死亡率.
- 在Gabra2-1小鼠中,产后 (+) -CBD-oct给药使异常树突性脊柱表型正常化.
结论:
- 具有延长基链的合成CBD同源物代表了新型抗药开发的有希望的途径.
- (+) -CBD-oct通过影响发作特征和大脑发育,证明了对发育性的治疗潜力.
- 基链长度是合成CBD同源的抗活性的一个关键因素.
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