Opioid Receptors

The opioid receptors were first demonstrated in 1973 with the binding of radiolabeled opiates to brain membranes. To date, three distinct families of opioid receptors have been identified that share many features. On the molecular level, they all are members of the G protein-coupled receptor family, which is a large family of receptors located within membranes. Members of this receptor family span the membrane seven times, providing both intracellular and extracellular domains (Fig. 3). The opioids and opioid peptides bind to the extracellular component of the receptor and activate G proteins inside the cell. The opioid receptors are almost exclusively coupled to inhibitory systems, primarily Go and G;. Each receptor is encoded by a separate gene, but there is high homology between them.

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