Department of Experimental Medicine, Tor Vergata University of Rome, Rome, Italy.
Methods Mol Biol. 2023;2576:95-109. doi: 10.1007/978-1-0716-2728-0_7.
Type-1 cannabinoid receptor (CB), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both the central nervous system and peripheral tissues. Today, its biochemical identification and pharmacological characterization, as well as the screening of thousands of novel ligands that might be useful for developing CB-based therapies, are the subject of intense research. Among available techniques that allow the analysis of CB binding activity, radioligand-based assays represent one of the best, fast, and reliable methods.Here, we describe radioligand binding methods standardized in our laboratory to assess CB binding in both tissues and cultured cells. We also report a high-throughput radioligand binding assay that allows to evaluate efficacy and potency of different compounds, which might represent the basis for the development of new drugs that target CB-dependent human diseases.
1 型大麻素受体（CB）是内源性大麻素的主要靶点之一，在影响中枢神经系统和外周组织的多种病理生理条件中发挥关键作用。如今，其生化鉴定和药理学特性，以及数千种新型配体的筛选，这些配体可能对开发基于 CB 的治疗方法有用，这是目前研究的热点。在允许分析 CB 结合活性的现有技术中，基于放射性配体的测定是最好、最快和最可靠的方法之一。在这里，我们描述了在我们实验室中标准化的放射性配体结合方法，以评估组织和培养细胞中的 CB 结合。我们还报告了一种高通量放射性配体结合测定法，可用于评估不同化合物的效力和效价，这可能为开发针对 CB 依赖性人类疾病的新药奠定基础。
