Zhang X, Bao L, Guan JS. Role of delivery and trafficking of δ-opioid receptors in opioid analgesia and tolerance. TRENDS IN PHARMACOLOGICAL SCIENCES 27(6): 324-329, 2006 (Review)

Abstract Changes in the number of receptors on the cell surface lead to modulations of physiological functions and pharmacological responses of neurons. Recent studies show that delta-opioid peptide (DOP) and mu-opioid peptide (MOP) receptors have distinct subcellular localizations in neurons. In nociceptive small neurons in the dorsal root ganglia, DOP receptors are sorted into neuropeptide-containing secretory vesicles, enabling the stimulus-induced cell surface expression of these receptors. MOP receptors are constitutively expressed on the cell surface. The physical interaction between DOP receptors and MOP receptors seems to be an important mechanism for the modulation of receptor functions. Experiments in animals show that MOP-receptor-mediated spinal analgesia is enhanced and morph......