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Figure 1 | Molecular Brain

Figure 1

From: Regulation of opioid receptor signalling: Implications for the development of analgesic tolerance

Figure 1

Steps involved in the homologous desensitization of GPCRs. According to the classical model of homologous desensitization, receptor activation by an agonist induces a series of conformational changes that trigger receptor signalling and regulation. The first of these regulatory steps is receptor phosphorylation by GRK (1). Once phosphorylated receptor affinity for ╬▓arrestin increases, enhancing interaction between the two proteins (2) and promoting internalization (3). Internalized receptors are then directed to early/sorting endodomes where interaction with different regulatory proteins will allow them to recycle back to the membrane (4) or will directed towards degradation (5).

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