Enhancement of morphine analgesic effect with induction of μ-opioid receptor endocytosis in rats
T Hashimoto, Y Saito, K Yamada, N Hara… - The Journal of the …, 2006 - pubs.asahq.org
Background Morphine can desensitize mu-opioid receptor (MOR), but it does not cause
internalization of the receptor after binding. Acute desensitization of MOR impairs the
efficiency of signaling, whereas the receptor internalization restores the cell responsiveness
to the agonists. Thereby, the property of morphine may limit the analgesic effects of this
opiate drug. It has been shown that [D-Ala2, MePhe4, Gly-ol5] enkephalin (DAMGO), a
potent MOR agonist inducing the internalization, facilitates morphine to internalize MOR …
internalization of the receptor after binding. Acute desensitization of MOR impairs the
efficiency of signaling, whereas the receptor internalization restores the cell responsiveness
to the agonists. Thereby, the property of morphine may limit the analgesic effects of this
opiate drug. It has been shown that [D-Ala2, MePhe4, Gly-ol5] enkephalin (DAMGO), a
potent MOR agonist inducing the internalization, facilitates morphine to internalize MOR …
