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Pharmacological Characterization of Receptor Redistribution and β-Arrestin Recruitment Assays for the Cannabinoid Receptor 1Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Invitrogen Discovery Sciences, Madison, Wisconsin
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands
Schering-Plough Research Institute, Molecular Pharmacology Unit, Oss, The Netherlands, guido.zaman{at}spcorp.com
Receptor redistribution and β-arrestin recruitment assays provide a G-protein-subtype-independent method to measure ligand-stimulated activation of G-protein-coupled receptors. In particular β-arrestin assays are becoming an increasingly popular tool for drug discovery. The authors have compared a high-content-imaging-based Redistribution® assay and 2 nonimaging-based β-arrestin recruitment assays, TangoTM and PathHunter TM, for the cannabinoid receptor 1. Inasmuch as all 3 assays use receptors that are modified at the C-terminus, the authors verified their pharmacology via detection of G
Key Words: cannabinoid receptor 1 • redistribution • β-arrestin recruitment
This version was published on August
1, 2009 Journal of Biomolecular Screening, Vol. 14, No. 7,
811-823 (2009) This article has been cited by other articles:
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i coupling of the receptor in cAMP assays using reference ligands. The potencies and efficacies of the cannabinoid receptor agonists CP55,940 and WIN55,212-2 correlated well between the 3 assays, and are comparable with the measured ligand binding affinities. The inverse agonist SR141716 decreased basal signal in all 3 assays, but only in the Tango bla assay a reliable EC50 could be determined for this compound, suggesting that Tango is the most suitable assay for the identification of new inverse agonists. Both the Redistribution and the PathHunter assay could discriminate partial agonists from full agonists, whereas in the Tango assay partial agonists behaved as full agonists. Only the PathHunter cells allowed detection of cannabinoid receptor activation via β-arrestin recruitment and G
