Desensitization of functional μ-opioid receptors increases agonist off-rate

Molecular Pharmacology

Volumn 86, Issue 1, 2014, Pages 52-61

  Williams, John T ^a  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBOXYNITROBENZYL TYROSINE LEUCINE 5 ENKEPHALIN; CARBOXYNITROVERATRYLNALOXONE; CHLORNALTREXAMINE; G PROTEIN COUPLED INWARDLY RECTIFYING POTASSIUM CHANNEL; LEUCINE ENKEPHALIN DERIVATIVE; MU OPIATE RECEPTOR; OPIATE AGONIST; POTASSIUM; UNCLASSIFIED DRUG; ENKEPHALIN; LIGAND; NALOXONE; NALTREXONE; NARCOTIC ANALGESIC AGENT;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN SLICE; CONTROLLED STUDY; DESENSITIZATION; DRUG RECEPTOR BINDING; LOCUS CERULEUS; NERVE CELL; NONHUMAN; PHOTOLYSIS; POTASSIUM CONDUCTANCE; POTASSIUM CURRENT; PRIORITY JOURNAL; RAT; REDUCTION; TIME; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; BRAIN; DRUG EFFECTS; KINETICS; METABOLISM;

ANALGESICS, OPIOID; ANIMALS; BRAIN; ENKEPHALINS; G PROTEIN-COUPLED INWARDLY-RECTIFYING POTASSIUM CHANNELS; KINETICS; LIGANDS; NALOXONE; NALTREXONE; PHOTOLYSIS; POTASSIUM; RATS; RECEPTORS, OPIOID, MU;

EID: 84901450816     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.114.092098     Document Type: Article

References (27)

1. Banghart MR and Sabatini BL (2012) Photoactivatable neuropeptides for spatiotemporally precise delivery of opioids in neural tissue. Neuron 73:249-259.
2. Banghart MR, Williams JT, Shah RC, Lavis LD, and Sabatini BL (2013) Caged naloxone reveals opioid signaling deactivation kinetics. Mol Pharmacol 84: 687-695.
3. Birdsong WT, Arttamangkul S, Clark MJ, Cheng K, Rice KC, Traynor JR, and Williams JT (2013) Increased agonist affinity at the m-opioid receptor induced by prolonged agonist exposure. J Neurosci 33:4118-4127.
4. Fiorillo CD and Williams JT (1996) Opioid desensitization: interactions with Gprotein- coupled receptors in the locus coeruleus. J Neurosci 16:1479-1485.
5. Ingram S, Wilding TJ, McCleskey EW, and Williams JT (1997) Efficacy and kinetics of opioid action on acutely dissociated neurons. Mol Pharmacol 52:136-143.
6. Just S, Illing S, Trester-Zedlitz M, Lau EK, Kotowski SJ, Miess E, Mann A, Doll C, Trinidad JC, and Burlingame AL et al. (2013) Differentiation of opioid drug effects by hierarchical multi-site phosphorylation. Mol Pharmacol 83:633-639.
7. Lau EK, Trester-Zedlitz M, Trinidad JC, Kotowski SJ, Krutchinsky AN, and Burlingame AL, von Zastrow M. (2011) Quantitative encoding of the effect of a partial agonist on individual opioid receptors by multisite phosphorylation and threshold detection. Cell Signal 4:ra52.
8. Levitt ES and Williams JT (2012) Morphine desensitization and cellular tolerance are distinguished in rat locus ceruleus neurons. Mol Pharmacol 82:983-992.
9. Llorente J, Lowe JD, Sanderson HS, Tsisanova E, Kelly E, Henderson G, and Bailey CP (2012) m-Opioid receptor desensitization: homologous or heterologous? Eur J Neurosci 36:3636-3642.
10. Lober RM, Pereira MA, and Lambert NA (2006) Rapid activation of inwardly rectifying potassium channels by immobile G-protein-coupled receptors. J Neurosci 26: 12602-12608.
11. Lohse MJ, Hein P, Hoffmann C, Nikolaev VO, Vilardaga JP, and BünemannM (2008) Kinetics of G-protein-coupled receptor signals in intact cells. Br J Pharmacol 153 (Suppl 1):S125-S132.
12. Nobles M, Benians A, and Tinker A (2005) Heterotrimeric G proteins precouple with G protein-coupled receptors in living cells. Proc Natl Acad Sci USA 102: 18706-18711.
13. Osborne PB and Williams JT (1995) Characterization of acute homologous desensitization of mu-opioid receptor-induced currents in locus coeruleus neurones. Br J Pharmacol 115:925-932.
14. Philip F, Sengupta P, and Scarlata S (2007) Signaling through a G Protein-coupled receptor and its corresponding G protein follows a stoichiometrically limited model. J Biol Chem 282:19203-19216.
15. Qin K, Dong C, Wu G, and Lambert NA (2011) Inactive-state preassembly of G(q)- coupled receptors and G(q) heterotrimers. Nat Chem Biol 7:740-747.
16. Qin K, Sethi PR, and Lambert NA (2008) Abundance and stability of complexes containing inactive G protein-coupled receptors and G proteins. FASEB J 22: 2920-2927.
17. Quillinan N, Lau EK, Virk M, von Zastrow M, and Williams JT (2011) Recovery from mu-opioid receptor desensitization after chronic treatment with morphine and methadone. J Neurosci 31:4434-4443.
18. Riven I, Iwanir S, and Reuveny E (2006) GIRK channel activation involves a local rearrangement of a preformed G protein channel complex. Neuron 51:561-573.
19. Scheibe SD, Bennett DB, Spain JW, Roth BL, and Coscia CJ (1984) Kinetic evidence for differential agonist and antagonist binding to bovine hippocampal synaptic membrane opioid receptors. J Biol Chem 259:13298-13303.
20. Vilardaga J-P (2010) Theme and variations on kinetics of GPCR activation/deactivation. J Recept Signal Transduct Res 30:304-312.
21. Virk MS, Arttamangkul S, Birdsong WT, and Williams JT (2009) Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci 29: 7341-7348.
22. Wang H-L, Chang W-T, Hsu C-Y, Huang P-C, Chow Y-W, and Li AH (2002) Identification of two C-terminal amino acids, Ser(355) and Thr(357), required for shortterm homologous desensitization of mu-opioid receptors. Biochem Pharmacol 64: 257-266.
23. Werling LL, Puttfarcken PS, and Cox BM (1988) Multiple agonist-affinity states of opioid receptors: regulation of binding by guanyl nucleotides in guinea pig cortical, NG108-15, and 7315c cell membranes. Mol Pharmacol 33:423-431.
24. Williams JT, Ingram SL, Henderson G, Chavkin C, von Zastrow M, Schulz S, Koch T, Evans CJ, and Christie MJ (2013) Regulation of m-opioid receptors: desensitization, phosphorylation, internalization, and tolerance. Pharmacol Rev 65: 223-254.
25. Williams JT and North RA (1984) Opiate-receptor interactions on single locus coeruleus neurones. Mol Pharmacol 26:489-497.
26. Zhang Q, Pacheco MA, and Doupnik CA (2002) Gating properties of GIRK channels activated by Galpha(o)- and Galpha(i)-coupled muscarinic m2 receptors in Xenopus oocytes: the role of receptor precoupling in RGS modulation. J Physiol 545: 355-373.
27. Zhou H, Chisari M, Raehal KM, Kaltenbronn KM, Bohn LM, Mennerick SJ, and Blumer KJ (2012) GIRK channel modulation by assembly with allosterically regulated RGS proteins. Proc Natl Acad Sci USA 109:19977-19982.