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用于合成大麻素结合动力学分析的表面等离子体共振(SPR):推进CB1受体相互作用研究

Surface Plasmon Resonance (SPR) for the Binding Kinetics Analysis of Synthetic Cannabinoids: Advancing CB1 Receptor Interaction Studies.

作者信息

Shi Xuesong, Kuai Lixin, Xu Deli, Qiao Yanling, Chen Yuanyuan, Di Bin, Xu Peng

机构信息

School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.

China Pharmaceutical University Joint Laboratory on Key Technologies of Narcotics Control, Office of China National Narcotics Control Commission, Beijing 100193, China.

出版信息

Int J Mol Sci. 2025 Apr 14;26(8):3692. doi: 10.3390/ijms26083692.

Abstract

Synthetic cannabinoids (SCs), a class of widely abused new psychoactive substances, are characterized by their structural diversity and rapid evolution. Structure-affinity relationships are crucial for predicting pharmacological effects and potential toxicity. Traditional methods for affinity testing are often complex and less applicable to newly modified compounds. In contrast, Surface Plasmon Resonance (SPR) is a sensitive and label-free technology that detects molecular interactions by measuring refractive index changes on a metallic surface with the advantages of high sensitivity, low sample consumption, and high-throughput capability. In this study, we used SPR to determine the receptor affinity constants of 10 SCs, including some first-reported substances, and analyzed their structure-affinity relationships to validate the method's reliability. The results showed that (1) indazole-based SCs exhibited stronger CB1 receptor affinity compared to their indole counterparts, (2) the head structure of p-fluorophenyl enhanced affinity relative to 5-fluoropentyl, (3) and the affinity rankings obtained from SPR experiments were consistent with those derived from traditional methods. These results collectively demonstrate the reliability and effectiveness of SPR in assessing CB1 receptor affinity and differentiating affinity differences among structurally similar analogs, with promising application prospects in drug research, particularly in the development and screening of therapeutic agents targeting cannabinoid receptors.

摘要

合成大麻素(SCs)是一类广泛滥用的新型精神活性物质,其特点是结构多样且快速演变。结构-亲和力关系对于预测药理作用和潜在毒性至关重要。传统的亲和力测试方法通常复杂,且不太适用于新修饰的化合物。相比之下,表面等离子体共振(SPR)是一种灵敏且无需标记的技术,通过测量金属表面的折射率变化来检测分子相互作用,具有高灵敏度、低样品消耗和高通量能力等优点。在本研究中,我们使用SPR测定了10种SCs(包括一些首次报道的物质)的受体亲和力常数,并分析了它们的结构-亲和力关系,以验证该方法的可靠性。结果表明:(1)与吲哚类合成大麻素相比,吲唑类合成大麻素表现出更强的CB1受体亲和力;(2)对氟苯基的头部结构相对于5-氟戊基增强了亲和力;(3)从SPR实验获得的亲和力排名与传统方法得出的结果一致。这些结果共同证明了SPR在评估CB1受体亲和力以及区分结构相似类似物之间的亲和力差异方面的可靠性和有效性,在药物研究中,尤其是在靶向大麻素受体的治疗剂的开发和筛选方面具有广阔的应用前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8888/12027443/eb37d928084a/ijms-26-03692-g001.jpg

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