The cannabinoid type 2 receptor (CB₂R) is an important therapeutic target for pain and inflammatory disorders. G protein-coupled receptors (GPCRs) are conventionally thought to signal exclusively at the plasma membrane; however, recently this has been challenged by the notion of intracellular signalling receptors. Better understanding of GPCR location requires tools that can differentiate cell surface versus subcellular receptors as well as accessing different parts of the body. Herein, we report the synthesis and pharmacological evaluation of polar chromenopyrazole-based CB₂R-selective agonists that contain short peptides that could be useful tools for interrogating CB₂R.

大麻素2型受体（CB ₂ R）是疼痛和炎性疾病的重要治疗靶标。通常认为，G蛋白偶联受体（GPCR）仅在质膜上发出信号。然而，近来这已经受到细胞内信号受体的观念的挑战。更好地理解GPCR的位置需要能够区分细胞表面和亚细胞受体以及进入身体不同部位的工具。在这里，我们报告的极性和基于苯并吡唑基的CB ₂ R选择性激动剂的合成和药理学评估，其中的短肽可能是询问CB ₂ R的有用工具。