(1) Background: The cannabinoid 2 receptor (CBR) is a promising anti-inflammatory drug target and development of selective CBR ligands may be useful for treating sight-threatening ocular inflammation. (2) Methods: This study examined the pharmacology of three novel chemically-diverse selective CBR ligands: CBR agonists, RO6871304, and RO6871085, as well as a CBR inverse agonist, RO6851228. In silico molecular modelling and cell-based receptor assays were used to verify CBR interactions, binding, cell signaling (ß-arrestin and cAMP) and early absorption, distribution, metabolism, excretion, and toxicology (ADMET) profiling of these receptor ligands.
View Article and Find Full Text PDFProliferative vitreoretinopathy (PVR) can develop after ocular trauma or inflammation and is a common complication of surgery to correct retinal detachment. Currently, there are no pharmacological treatments for PVR. Cannabinoids acting at cannabinoid 2 receptor (CB2R) can decrease inflammation and fibrosis.
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