Cannabinoids have emerged on the national scene as a promising untapped therapeutic class. In pursuit of development of cannabinoids for pharmacologic use, I established and validated two high-throughput in vitro pharmacological screening systems, the ACTOne cannabinoid 1 and cannabinoid 2 assays, to aid in evaluating cannabinoid compounds for receptor affinity, pharmacologic potency and efficacy, and for selected compounds, antagonist activity. Our lead compound, SMM-189, was evaluated using the ACTOne assays and determined to be a CB2 inverse agonist. Further investigation revealed SMM-189 to exert anti-inflammatory effects on the brain’s immune cells, microglia, through polarization to a pro-wound healing state. Next generation analogs of SMM-189 were also evaluated in the ACTOne assays in the hopes of developing a molecule with improved biochemical characteristics
