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Vol. 53, Issue 3, 377-384, March 1998
Department of Psychiatry and Biobehavioral Sciences (D.E.K., B.A.,
P.A.Z., G.M.-A., C.J.E.),
University of California, Los Angeles, and
Department of Molecular and Medical Pharmacology (P.L.S.), Crump
Institute for Biological Imaging, University of California, Los
Angeles, School of Medicine, Los Angeles, California 90095-1770, and
Departments of
Psychiatry and Cellular and Molecular Pharmacology and
Center for Neurobiology and Psychiatry (S.R.M., P.C.C., D.V.L.,
M.v.Z.), University of California, San Francisco, San Francisco, CA
94143
µ-Opioid receptors are the pharmacological targets of endogenous
opioid peptides and morphine-like alkaloid drugs. Previous studies of
transfected cells and peripheral neurons indicate that opioid receptors
are rapidly internalized after activation by the alkaloid agonist
etorphine but not after activation by morphine. To determine whether
opioid receptors in the central nervous system are regulated by a
similar process of agonist-selective internalization, µ-opioid
receptors were examined in rat brain neurons after treatment of animals
with opioid drugs. Internalized µ receptors were observed within 30 min after intraperitoneal injection of the alkaloid agonist etorphine,
and this process was blocked by the antagonist naloxone. Colocalization
of internalized opioid receptors with transferrin receptors in confocal
optical sections indicated that receptor internalization observed
in vivo is mediated by a membrane trafficking pathway
similar to that observed previously in vitro using
transfected human embryonic kidney 293 cells. Morphine failed to induce
detectable rapid internalization of receptors, even when administered
to animals at doses far in excess of those required to induce
analgesia. To quantify these agonist-selective differences and to
analyze an array of opioid ligands for their ability to trigger
internalization, we used flow cytometry on stably transfected 293 cells. These studies indicated that the different effects of individual
agonists are not correlated with their potencies for receptor
activation and that a variety of clinically important agonists differ
significantly in their relative abilities to stimulate the rapid
internalization of opioid receptors.
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J. L. Whistler and M. von Zastrow Morphine-activated opioid receptors elude desensitization by beta -arrestin PNAS, August 18, 1998; 95(17): 9914 - 9919. [Abstract] [Full Text] [PDF]
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K. Chaturvedi, P. Bandari, N. Chinen, and R. D. Howells Proteasome Involvement in Agonist-induced Down-regulation of {micro} and delta Opioid Receptors J. Biol. Chem., April 6, 2001; 276(15): 12345 - 12355. [Abstract] [Full Text] [PDF]
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R. El Kouhen, A. L. Burd, L. J. Erickson-Herbrandson, C.-Y. Chang, P.-Y. Law, and H. H. Loh Phosphorylation of Ser363, Thr370, and Ser375 Residues within the Carboxyl Tail Differentially Regulates {micro}-Opioid Receptor Internalization J. Biol. Chem., April 13, 2001; 276(16): 12774 - 12780. [Abstract] [Full Text] [PDF]
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