Patent ID: 7297503

Claim:
A method of identifying a G protein-coupled receptor (GPCR) agonist, wherein the GPCR agonist is capable of activating GPCR signaling while exhibiting reduced GPCR internalization as compared to a control compound, comprising the steps of: (a) providing a cell comprising at least one GPCR or a modified GPCR capable of activating intracellular signaling and an arrestin, or a fragment thereof capable of binding a GPCR, (b) exposing the cell to at least one test compound, (c) measuring GPCR signaling at two or more points in time, (d) measuring internalization of the GPCR at two or more points in time, (e) quantitatively determining if GPCR internalization is reduced by comparing GPCR internalization in the presence of the test compound to GPCR internalization in the presence of a control compound, and wherein-GPCR signaling is activated in the presence of the test compound as compared to GPCR signaling in the absence of the test compound, (f) wherein a reduction in GPCR internalization in the presence of the test compound as compared to the control compound indicates the test compound is a GPCR agonist capable of activating GPCR signaling while exhibiting reduced GPCR internalization.