Assessment of Biased Agonism among Distinct Synthetic Cannabinoid Receptor Agonist Scaffolds.

ABSTRACT: Cannabinoid receptor 1 (CB1) is a key drug target for a number of diseases, including metabolic syndromes and neuropathic pain. Most of the typical cannabinoid ligands provoke psychotropic side effects that impair their therapeutic utility. As of today, it is not yet clearly known which structural features of cannabinoid ligands determine a preference toward specific signaling pathways. Distinct bioassays are typically used to elucidate signaling preferences. However, these are often based on different cell lines and use different principles and/or read-outs, which makes straightforward assessment of "ligand bias" difficult. Within this context, this study is the first to investigate ligand bias among synthetic cannabinoid receptor agonists (SCRAs) in as closely analogous conditions as pos

SUBMITTER: Wouters E 

PROVIDER: S-EPMC7155187 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature