In vitro determination of the efficacy of illicit synthetic cannabinoids at CB₁ receptors.

ABSTRACT:

Background and purpose

The morbidity and mortality associated with recreational use of synthetic cannabinoid receptor agonists (SCRAs) may reflect strong activation of CB₁ receptors and is a major health concern. The properties of SCRA at CB₁ receptors are not well defined. Here we have developed an assay to determine acute CB₁ receptor efficacy using receptor depletion with the irreversible CB₁ receptor antagonist AM6544, with application of the Black and Leff operational model to calculate efficacy.

Experimental approach

Receptor depletion in mouse AtT-20 pituitary adenoma cells stably expressing human CB₁ receptors was achieved by pretreatment of cells with AM6544 (10 μM, 60 min). The CB₁ receptor-mediated

SUBMITTER: Sachdev S 

PROVIDER: S-EPMC6965679 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature