J.L. and J.D.L. contributed equally to this study.
Research Report
μ-Opioid receptor desensitization: homologous or heterologous?
Article first published online: 24 SEP 2012
DOI: 10.1111/ejn.12003
© 2012 Federation of European Neuroscience Societies and Blackwell Publishing Ltd
Additional Information
How to Cite
Llorente, J., Lowe, J. D., Sanderson, H. S., Tsisanova, E., Kelly, E., Henderson, G. and Bailey, C. P. (2012), μ-Opioid receptor desensitization: homologous or heterologous?. European Journal of Neuroscience, 36: 3636–3642. doi: 10.1111/ejn.12003
- ‡
J.L. and J.D.L. contributed equally to this study.
Re-use of this article is permitted in accordance with the Terms and Conditions set out at http://wileyonlinelibrary.com/onlineopen#OnlineOpen_Terms
Publication History
- Issue published online: 17 DEC 2012
- Article first published online: 24 SEP 2012
- Manuscript Accepted: 15 AUG 2012
- Manuscript Revised: 14 AUG 2012
- Manuscript Received: 8 MAY 2012
Funded by
- National Institute on Drug Abuse (USA) international collaboration. Grant Number: DA 020836
- Medical Research Council (UK). Grant Number: G0701486
- Wellcome Trust
References
- , , , , , , & (2002) μ-Opioid receptors: ligand-dependent activation of potassium conductance, desensitization, and internalization. J. Neurosci., 22, 5769–5776.
- , , & (2012) Desensitization and trafficking of μ-opioid receptors in locus ceruleus neurons: modulation by kinases. Mol. Pharmacol., 81, 348–355.
- , & (2004) Protein kinase C activation enhances morphine-induced rapid desensitization of μ-opioid receptors in mature rat locus ceruleus neurons. Mol. Pharmacol., 66, 1592–1598.
- , , , & (2006) How important is protein kinase C in μ-opioid receptor desensitization and morphine tolerance? Trends Pharmacol. Sci., 27, 558–565.
- , , , , , , , , , & (2009) Involvement of PKC alpha and G-protein-coupled receptor kinase 2 in agonist-selective desensitization of μ-opioid receptors in mature brain neurons. Br. J. Pharmacol., 158, 157–164.
- & (2002) Desensitization of μ-opioid receptor-evoked potassium currents: initiation at the receptor, expression at the effector. Proc. Natl. Acad. Sci. USA, 99, 4674–4679.
- , , & (1996) Operational characteristics of somatostatin receptors mediating inhibitory actions on rat locus coeruleus neurones. Br. J. Pharmacol., 117, 1673–1678.
- , & (1987) Cellular mechanisms of opioid tolerance: studies in single brain neurons. Mol. Pharmacol., 32, 633–638.
- , & (1989) Electrical coupling synchronizes subthreshold activity in locus coeruleus neurons in vitro from neonatal rats. J. Neurosci., 9, 3584–3589.
- , & (1997) Cortistatin increase of a potassium conductance in rat locus coeruleus in vitro. Br. J. Pharmacol., 122, 1567–1572.
- & (2012) Mechanisms of rapid opioid receptor desensitization, resensitization and tolerance in brain neurons. Br. J. Pharmacol., 165, 1704–1716.
- , & (2009) Two distinct mechanisms mediate acute μ-opioid receptor desensitization in native neurons. J. Neurosci., 29, 3322–3327.
- , & (2012) Prolonged stimulation of μ-opioid receptors produces β-arrestin-2 mediated heterologous desensitization of α2-adrenoceptor function in locus coeruleusneurons. Mol. Pharmacol., 82, 473–480.
- , , , , , , , , , , & (2011) Analgesic tolerance to high-efficacy agonists but not to morphine is diminished in phosphorylation-deficient S375A μ-opioid receptor knock-in mice. J. Neurosci., 31, 13890–13896.
- & (1991) Transient homologous μ-opioid receptor desensitization in rat locus coeruleus neurons. J. Neurosci., 11, 2574–2581.
- & (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry, 38, 14286–14293.
- , , , , , , , , & (2006) Agonist-selective mechanisms of μ-opioid receptor desensitization in human embryonic kidney 293 cells. Mol. Pharmacol., 70, 676–685.
- , & (2008) Agonist selective mechanisms of GPCR desensitization. Br. J. Pharmacol., 153, S379–S388.
- , , , , , & (2011) Quantitative encoding of the effect of a partial agonist on individual opioid receptors by multisite phosphorylation and threshold detection. Sci. Signal., 4, ra52.
- , & (2011) Gi/o-coupled receptors compete for signaling to adenylyl cyclase in SH-SY5Y cells and reduce opioid-mediated cAMP overshoot. Mol. Pharmacol., 79, 461–471.
- , , & (2010) Ligand-directed c-Jun N-terminal kinase activation disrupts opioid receptor signaling. Proc. Natl. Acad. Sci. USA, 107, 11608–11613.
- & (1985) On the potassium conductance increased by opioids in rat locus coeruleus neurones. J. Physiol., 364, 265–280.
- & (1995) Characterization of acute homologous desensitization of μ-opioid receptor-induced currents in locus coeruleus neurons. Br. J. Pharmacol., 115, 925–932.
- , , & (2000) Expression patterns of the regulatory proteins G protein-coupled receptor kinase 2 and β-arrestin 1 during rat postnatal brain development. Eur. J. Biochem., 267, 4390–4396.
- , , , & (2011) Recovery from μ-opioid receptor desensitization after chronic treatment with morphine and methadone. J. Neurosci., 31, 4434–4443.
- , , & (2010) Nonenzymatic rapid control of GIRK channel function by a G protein-coupled receptor kinase. Cell, 143, 750–760.
- , , , , & (2003) Phosphoinositide 3-kinase cascade facilitates μ-opioid desensitization in sensory neurons by altering G-protein-effector interactions. J. Neurosci., 23, 10292–10301.
- , , & (2009) p38 MAPK and beta-arrestin 2 mediate functional interactions between endogenous μ-opioid and alpha2A-adrenergic receptor in neurons. J. Biol. Chem., 284, 6270–6281.
- , , , , , & (2006) Mu opioid receptor-effector coupling and trafficking in dorsal root ganglia neurons. Neuroscience, 142, 493–503.

1460-9568/asset/EJN_left.gif?v=1&s=3d5223e01f3255a775e3d3fc8d54bc1c38677c6c)
