关键词: Cannabinoids Drug repurposing Functional interaction Synthetic cannabinoids

Mesh : Cannabinoids / pharmacology chemistry Humans Animals Structure-Activity Relationship Receptors, Cannabinoid / metabolism Ligands Cannabinoid Receptor Agonists / pharmacology chemistry

来  源:   DOI:10.1016/j.ejphar.2024.176679

Abstract:
To provide a comprehensive framework of the current information on the potency and efficacy of interaction between phyto- and synthetic cannabinoids and their respective receptors, an electronic search of the PubMed, Scopus, and EMBASE literature was performed. Experimental studies included reports of mechanistic data providing affinity, efficacy, and half-maximal effective concentration (EC50). Among the 108 included studies, 174 structures, and 16 targets were extracted. The most frequent ligands belonged to the miscellaneous category with 40.2% followed by phytocannabinoid-similar, indole-similar, and pyrrole-similar structures with an abundance of 17.8%, 16.6%, and 12% respectively. 64.8% of structures acted as agonists, 17.1 % appeared as inverse agonists, 10.8% as antagonists, and 7.2% of structures were reported with antagonist/inverse agonist properties. Our outcomes identify the affinity, EC50, and efficacy of the interactions between cannabinoids and their corresponding receptors and the subsequent response, evaluated in the available evidence. Considering structures\' significance and very important effects of on the activities, the obtained results also provide clues to drug repurposing.
摘要:
为了提供有关植物和合成大麻素及其各自受体之间相互作用的效力和功效的当前信息的综合框架,对PubMed的电子搜索,Scopus,并进行了EMBASE文献。实验研究包括提供亲和力的机械数据报告,功效,和半最大有效浓度(EC50)。在纳入的108项研究中,174个结构,并提取了16个目标。最常见的配体属于杂类,40.2%,其次是植物大麻素相似,吲哚相似,和吡咯相似的结构,丰度为17.8%,16.6%,分别为12%。64.8%的结构作为激动剂,17.1%出现为反向激动剂,10.8%作为拮抗剂,据报道,7.2%的结构具有拮抗剂/反激动剂特性。我们的结果确定了亲和力,EC50,以及大麻素与其相应受体之间的相互作用以及随后的反应的功效,在现有证据中进行评估。考虑到结构的重要性和对活动的非常重要的影响,获得的结果也为药物的再利用提供了线索。
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