Xie2-64, a novel CB₂ receptor inverse agonist, reduces cocaine abuse-related behaviors in rodents.

ABSTRACT: Cocaine abuse remains a public health threat around the world. There are no pharmacological treatments approved for cocaine use disorder. Cannabis has received growing attention as a treatment for many conditions, including addiction. Most cannabis-based medication development has focused on cannabinoid CB₁ receptor (CB₁R) antagonists (and also inverse agonists) such as rimonabant, but clinical trials with rimonabant have failed due to its significant side-effects. Here we sought to determine whether a novel and selective CB₂R inverse agonist, Xie2-64, has similar therapeutic potential for cocaine use disorder. Computational modeling indicated that Xie2-64 binds to CB₂R in a way similar to SR144528, another well-characterized but less selective C

SUBMITTER: Jordan CJ 

PROVIDER: S-EPMC7529998 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature