Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid, leukotriene, bile acid, and platelet-activating factor receptor families are class A G protein–coupled receptors with endogenous lipid ligands. Pharmacological tools are crucial for studying these receptors and addressing the many unanswered questions surrounding expression of these receptors in normal and diseased tissues. An inherent challenge for developing tools for these lipid receptors is balancing the often lipophilic requirements of the receptor-binding pharmacophore with favorable physicochemical properties to optimize highly specific binding. In this study, we review the radioligands, fluorescent ligands, covalent ligands, and antibodies that have been used to study these lipid-binding receptors. For each tool type, the characteristics and design rationale along with in vitro and in vivo applications are detailed.

大麻素，游离脂肪酸，溶血磷脂酸，1-磷酸鞘氨醇，前列腺素，白三烯，胆汁酸和血小板活化因子受体家族是具有内源性脂质配体的AG类蛋白偶联受体。药理学工具对于研究这些受体并解决围绕正常和患病组织中这些受体表达的许多未解决问题至关重要。开发用于这些脂质受体的工具的固有挑战是平衡受体结合药效团的亲脂性要求与有利的理化性质以优化高度特异性结合。在这项研究中，我们回顾了用于研究这些脂质结合受体的放射性配体，荧光配体，共价配体和抗体。对于每种工具类型，