Abstract
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.