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Journal of Biomolecular Screening
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Pharmacological Comparison of a Recombinant CB1 Cannabinoid Receptor with Its Ga16 Fusion Product

Renée S. Martin

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Paul H. Reynen

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Joyce J. Calixto

Theravance, Inc., South San Francisco, CA

Christian L. Reyes

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Thomas K. Chang

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Paul S. Dietrich

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Douglas W. Bonhaus

Neurobiology Unit, Roche Bioscience, Palo Alto, CA

Stephen J. Maclennan

0SI Pharmaceuticals, Inc., Tarrytown, NY

The pharmacology of G protein-coupled receptors is widely accepted to depend on the G protein subunit to which the agonist-stimulated receptor couples. In order to investigate whether CB1 agonist-mediated signal transduction via an engineered Ga{alpha}16 system is different than that of the Gi/o coupling normally preferred by the CB1 receptor, we transfected the human recombinant CB1 receptor (hCB1) or a fusion protein comprising the hCB1 receptor and G{alpha}16 (hCB1-G{alpha}16) into HEK293 cells. From competition binding studies, the rank order of ligand affinities at the hCB1-Ga{alpha}16 fusion protein was found to be similar to that for hCB1: HU 210 > CP 55,940 ≥ SR 141716A > WIN 55212-2 > anandamide > JWH 015. Agonists increased [35S]GTP{gamma}S binding or inhibited forskolin-stimulated cAMP, presumably by coupling to Gi/o, in cells expressing hCB1 but not hCB1-G{alpha}16. However, an analogous rank order of potencies was observed for these agonists in their ability to evoke increases in intracellular calcium concentration in cells expressing hCBq-Ga{alpha}16 but not hCB1. These data demonstrate that ligand affinities for the hCB1, receptor are not affected by fusion to the G{alpha}16 subunit. Furthermore, there is essentially no difference in the function of the hCB1, receptor when coupled to Gi/o, or G{alpha}16.

Journal of Biomolecular Screening, Vol. 7, No. 3, 281-289 (2002)
DOI: 10.1177/108705710200700312
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A. M.F. Liu, M. K.C. Ho, C. S.S. Wong, J. H.P. Chan, A. H.M. Pau, and Y. H. Wong
G{alpha} 16/z Chimeras Efficiently Link a Wide Range of G Protein-- Coupled Receptors to Calcium Mobilization
J Biomol Screen, January 1, 2003; 8(1): 39 - 49.
[Abstract] [PDF]