CBD与CBDP:比较体外受体结合活动
Mehdi Haghdoost1, Scott Young2, Alisha K Holloway3
1Nalu Bio Inc., 38 Keyes Avenue, Suite 117, San Francisco, CA 94129, USA.
International journal of molecular sciences
|July 27, 2024
概括
大麻二醇 (CBDP) 和大麻二醇 (CBD) 具有相似的活性,而CBD是一个略强的CB2受体对手. 意想不到的是,CBDP与CBD不同,在片受体中充当积极的全调节器.
科学领域:
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
- 分子生物学分子生物学
背景情况:
- 具有七碳基链 (醇) 的植物性大麻素,如大麻二醇 (CBDP),因其被认为比较短链的类似物具有更高的功效而引起了人们的注意.
- 大麻二醇 (CBDP) 和四大麻二醇 (THCP) 在商业上可用,但它们的生物活性在很大程度上仍未被描述.
研究的目的:
- 研究与大麻 (CBD) 相比,CBDP的体外受体结合活性和相对强度.
- 探索CBDP与大麻素,血清素和阿片类受体的相互作用.
主要方法:
- 在体外受体结合实验中,评估CBDP在CB1 / CB2受体的对抗性,在5HT-1A和多巴胺D2S受体的对抗性,以及在片受体的调制性.
- 放射性配体结合试验用于确定主要的生物标.
- 分子对接模拟以阐明受体相互作用的结构机制.
主要成果:
- CBDP和CBD表现出类似的活性概况,CBD显示出作为CB2受体对手的强度略大 (p <0.05).
- 鉴定出CB2受体可能是CBDP的主要点,尽管这两种大麻素的效果不如SR144528.
- CBDP在片受体上表现出意想不到的正调节器 (PAM) 活性,与大麻素的预期负调节器 (NAM) 作用形成鲜明对比.
结论:
- 与预期相反,CBDP本质上并不比CBD更强大,并且在片受体上表现出明显的相互作用概况.
- 分子对接表明CBDP和met-enkephalin与mu-opioid受体的联合结合,解释了观察到的PAM效应.
- 需要进一步的研究才能充分理解CBDP独特受体相互作用的药理学影响.
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