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Agonist functional selectivity and GPCR desensitization Agonist activation of a GPCR-mediated response has generally been viewed in ‘linear' terms, that is, the various agonists that activate a particular GPCR do so by stabilizing the same activated conformation of the receptor, which then couples to the same G protein or set of G proteins (or even non-G protein effectors) and hence activate or inhibit the same set of intracellular responses (Figure 2a)
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