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Journal of Biomolecular Screening
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Characterizing Cannabinoid CB2 Receptor Ligands Using DiscoveRx PathHunterTM β-Arrestin Assay

Debra Mcguinness

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Asra Malikzay

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Richard Visconti

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Karen Lin

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Marvin Bayne

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Frederick Monsma

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey

Charles A. Lunn

New Lead Discovery, Schering-Plough Research Institute, Kenilworth, New Jersey, charles.lunn{at}spcorp.com

The authors have characterized a set of cannabinoid CB2 receptor ligands, including triaryl bis sulfone inverse agonists, in a cell-based receptor/β-arrestin interaction assay (DiscoveRx PathHunterTM). The results were compared with results using a competitive ligand binding assay, and with effects on forskolin-stimulated cAMP levels (PerkinElmer LANCETM). The authors show good correlation between the 3 assay systems tested, with the β-arrestin protein complementation assay exhibiting a more robust signal than the cAMP assay for cannabinoid CB2 agonists. Further assay validation shows that DiscoveRx PathHunterTM HEK293 CB2 β-arrestin assay can be carried out from cryopreserved cell suspensions, eliminating variations caused by the need for multiple cell pools during live cell screening campaigns. These results, and the authors' results evaluating a test set of random library compounds, validate the use of ligand-induced interaction between the human cannabinoid CB2 receptor and β-arrestin as an appropriate and valuable screening platform for compounds specific for the cannabinoid CB2 receptor. (Journal of Biomolecular Screening 2009:49-58)

Key Words: cannabinoid CB2 receptor • β-arrestin • complementation • signal transduction

Journal of Biomolecular Screening, Vol. 14, No. 1, 49-58 (2009)
DOI: 10.1177/1087057108327329
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