A continuous, fluorescence-based assay of μ-opioid receptor activation in AtT-20 cells

Journal of Biomolecular Screening

Volumn 18, Issue 3, 2013, Pages 269-276

  Knapman, Alisa ^a   Santiago, Marina ^a   Du, Yan Ping ^b   Bennallack, Philip R ^a,c   Christie, MacDonald J ^b   Connor, Mark ^a  

^a MACQUARIE UNIVERSITY   (Australia)

^b UNIVERSITY OF SYDNEY   (Australia)

^c BRIGHAM YOUNG UNIVERSITY   (United States)

Author keywords

cell based assay; fluorescence; GIRK channels; high throughput screening; opioids

Indexed keywords

BETA ENDORPHIN; BUPRENORPHINE; ENDOMORPHIN 1; ENDOMORPHIN 2; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; FENTANYL; G PROTEIN COUPLED INWARDLY RECTIFYING POTASSIUM CHANNEL; METENKEPHALIN; METHADONE; MORPHINE; MU OPIATE RECEPTOR; NALOXONE; OXYCODONE; PENTAZOCINE; PERTUSSIS TOXIN;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL ASSAY; FLUORESCENCE ANALYSIS; HIGH THROUGHPUT SCREENING; MEMBRANE POTENTIAL; MOUSE; NONHUMAN; PRIORITY JOURNAL; RECEPTOR DOWN REGULATION;

ANALGESICS, OPIOID; ANIMALS; DRUG TOLERANCE; FLUORESCENCE; GTP-BINDING PROTEINS; HIGH-THROUGHPUT SCREENING ASSAYS; LIGANDS; MEMBRANE POTENTIALS; MICE; MORPHINE; NALOXONE; NEUROBLASTOMA; PERTUSSIS TOXIN; POTASSIUM CHANNELS; RECEPTORS, OPIOID, MU; TUMOR CELLS, CULTURED;

EID: 84873629222     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057112461376     Document Type: Article

References (36)

1. Buntin-Mushock C., Phillip L., Moriyama K., Palmer P. P.. Age-Dependent Opioid Escalation in Chronic Pain Patients. Anesth. Analg. 2005 ; 100: 1740-1745 (Pubitemid 40712733)
2. Matthes H. W. D., Maldonado R., Simonin F., Valverde O., Slowe S., Kitchen I., Befort K., Dierich A., Le Meur M., Dolle P., et al. Loss of Morphine-Induced Analgesia, Reward Effect and Withdrawal Symptoms in Mice Lacking the μ-Opioid-Receptor Gene. Nature. 1996 ; 383: 819-823
3. Alexander S. P. H., Mathie A., Peters J. A.. Guide to Receptors and Channels (GRAC). Br. J. Pharmacol. 2011 ; 164: S1 - S324
4. Law P. Y., Wong Y. H., Loh H. H.. Molecular Mechanisms and Regulation of Opioid Receptor Signaling. Ann. Rev. Pharmacol. Toxicol. 2000 ; 40: 389-430 (Pubitemid 30340688)
5. Rajagopal S., Rajagopal K., Lefkowitz R. J.. Teaching Old Receptors New Tricks: Biasing Seven-Transmembrane Receptors. Nat. Rev. Drug Discov. 2010 ; 9: 373-386
6. Bailey C. P., Llorente J., Gabra B. H., Smith F. L., Dewey W. L., Kelly E., Henderson G.. Role of Protein Kinase C and mu-Opioid Receptor (MOPr) Desensitization in Tolerance to Morphine in Rat Locus Coeruleus Neurons. Eur. J. Neurosci. 2009 ; 29: 307-318
7. Connor M., Osborne P. B., Christie M. J.. mu-Opioid Receptor Desensitization: Is Morphine Different?. Br. J. Pharmacol. 2004 ; 143: 685-696 (Pubitemid 39611604)
8. Pradhan A. A., Walwyn W., Nozaki C., Filliol D., Erbs E., Matifas., Evans C., Kieffer B. L.. Ligand-Directed Trafficking of the Delta-Opioid Receptor In Vivo: Two Paths toward Analgesic Tolerance. J. Neurosci. 2010 ; 30: 16459-16468
9. Coward P., Chan S. D. H., Wada H. G., Humphries G. M., Conklin B. R.. Chimeric G-Proteins Allow a High-Throughput Signaling Assay of Gi-Coupled Receptors. Anal. Biochem. 1999 ; 270: 242-248 (Pubitemid 29252535)
10. Hill S. J., Williams C., May L. T.. Insights into GPCR Pharmacology from the Measurement of Changes in Intracellular Cyclic AMP: Advantages and Pitfalls of Differing Methodologies. Br. J. Pharmacol. 2010 ; 161: 1266-1275
11. Borgland S. L., Connor M., Osborne P. B., Furness J. B., Christie M. J.. Opioid Agonists Have Different Efficacy Profiles for G Protein Activation, Rapid Desensitization, and Endocytosis of mu-Opioid Receptors. J. Biol. Chem. 2003 ; 278: 18776-18784 (Pubitemid 36799259)
12. Celver J., Xu M., Jin W., Lowe J., Chavkin C.. Distinct Domains of the μ-Opioid Receptor Control Uncoupling and Internalization. Mol. Pharmacol. 2004 ; 65: 528-537 (Pubitemid 38264020)
13. Zhang J.-H., Chung T. D. Y., Oldenburg K. R.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999 ; 4: 67-73 (Pubitemid 29278954)
14. Kaufman D. L., Keith D. L., Anton B., Tian J., Magendzo K., Newman D., Tran T. H., Lee D. S., Wen C., Xia Y.-R., et al. Characterization of the Murine μ-Opioid Receptor Gene. J. Biol. Chem. 1995 ; 270: 15877-15883
15. Cervia D., Nunn C., Fehlmann D., Langenegger D., Schuepbach E., Hoyer D.. Pharmacological Characterisation of Native Somatostatin Receptors in AtT-20 Mouse Tumour Corticotrophs. Br. J. Pharmacol. 2003 ; 139: 109-121 (Pubitemid 36645314)
16. Doebler J. A.. Comparative Effects of Carboxylic Ionophores on Membrane Potential and Resistance of NG108-15 Cells. Toxicol. In Vitro. 2000 ; 14: 235-243 (Pubitemid 30235121)
17. Pepper C. M., Henderson G.. Opiates and Opioid Peptides Hyperpolarize Locus Coeruleus Neurons In Vitro. Science. 1980 ; 209: 394-395
18. Connor M., Schuller A., Pintar J. E., Christie M. J.. μ-Opioid Receptor Modulation of Calcium Channel Current in Periaqueductal Grey Neurons from C57B16/J Mice and Mutant Mice Lacking MOR-1. Br. J. Pharmacol. 1999 ; 126: 1553-1558 (Pubitemid 29182338)
19. Christie M. J., Williams J. T., North R. A.. Cellular Mechanisms of Opioid Tolerance: Studies in Single Brain Neurons. Mol. Pharmacol. 1987 ; 32: 633-638 (Pubitemid 18004177)
20. Ingram S., Wilding T. J., McCleskey E. W., Williams J. T.. Efficacy and Kinetics of Opioid Action on Acutely Dissociated Neurons. Mol. Pharmacol. 1997 ; 52: 136-143 (Pubitemid 27318629)
21. Alt A., Mansour A., Akil H., Medzihradsky F., Traynor J. R., Woods J. H.. Stimulation of Guanosine-5′-O-(3-[35S]Thio)Triphosphate Binding by Endogenous Opioids Acting at a Cloned mu-Receptor. J. Pharmacol. Exp. Ther. 1998 ; 286: 282-288 (Pubitemid 28318001)
22. Rodriguez-Martin I., Braksator E., Bailey C. P., Goodchild S., Marrion N. V., Kelly E., Henderson G.. Methadone: Does It Really Have Low Efficacy at μ-Opioid Receptors?. Neuroreport. 2008 ; 19: 589-593 (Pubitemid 351501473)
23. Selley D. E., Liu Q., Childers S. R.. Signal Transduction Correlates of mu Opioid Agonist Intrinsic Efficacy: Receptor-Stimulated [35S]GTPγS Binding in mMOR-CHO Cells and Rat Thalamus. J. Pharmacol. Exp. Ther. 1998 ; 285: 496-505 (Pubitemid 28237424)
24. Matsui A., Williams J. T.. Activation of μ-Opioid Receptors and Block of KIR3 Potassium Channels and NMDA Receptor Conductance by l- and d-Methadone in Rat Locus Coeruleus. Br. J. Pharmacol. 2010 ; 161: 1403-1413
25. McPherson J., Rivero G., Baptist M., Llorente J., Al-Sabah S., Krasel C., Dewey W. L., Bailey C. P., Rosethorne E. M., Charlton S. J., et al. μ-Opioid Receptors: Correlation of Agonist Efficacy for Signaling with Ability to Activate Internalization. Mol. Pharm. 2010 ; 78: 756-766
26. Rivero G., Llorente J., McPherson J., Cooke A., Mundell S. J., McArdle C. A., Rosethorne E. M., Charlton S. J., Krasel C., Bailey C. P., et al. Endomorphin-2: A Biased Agonist at the μ-Opioid Receptor. Mol. Pharm. 2012 ; 82: 178-188
27. Harris G., Williams J.. Transient Homologous mu-Opioid Receptor Desensitization in Rat Locus Coeruleus Neurons. J. Neurosci. 1991 ; 11: 2574-2581
28. Johnson E. A., Oldfield S., Braksator E., Gonzalez-Cuello A., Couch D., Hall K. J., Mundell S. J., Bailey C. P., Kelly E., Henderson G.. Agonist-Selective Mechanisms of mu-Opioid Receptor Desensitization in Human Embryonic Kidney 293 Cells. Mol. Pharmacol. 2006 ; 70: 676-685 (Pubitemid 44092328)
29. Niswender C. M., Johnson K. A., Luo Q., Ayala J. E., Kim C., Conn P. J., Weaver C. D.. A Novel Assay of Gi/o-Linked G Protein-Coupled Receptor Coupling to Potassium Channels Provides New Insights into the Pharmacology of the Group III Metabotropic Glutamate Receptors. Mol. Pharmacol. 2008 ; 73: 1213-1224 (Pubitemid 351439203)
30. Walsh K. B.. A Real-Time Screening Assay for GIRK1/4 Channel Blockers. J. Biomol. Screen. 2010 ; 15: 1229-1237
31. Walsh K. B.. Targeting GIRK Channels for the Development of New Therapeutic Agents. Front. Pharmacol. 2011 ; 2: 1-8
32. Wolff C., Fuks B., Chatelain P.. Comparative Study of Membrane Potential-Sensitive Fluorescent Probes and Their Use in Ion Channel Screening Assays. J. Biomol. Screen. 2003 ; 8: 533-543
33. Harrison C., Traynor J. R.. The [35S]GTPγS Binding Assay: Approaches and Applications in Pharmacology. Life Sci. 2003 ; 74: 489-508 (Pubitemid 37377904)
34. Connor M. A., Keir M. J., Henderson G.. δ-Opioid Receptor Mobilization of Intracellular Calcium in SH-SY5Y Cells: Lack of Evidence for δ-Receptor Subtypes. Neuropharmacology. 1997 ; 36: 125-133 (Pubitemid 27115850)
35. Chu J., Zheng H., Zhang Y. H., Loh H. H., Law P. Y.. Agonist-Dependent mu-Opioid Receptor Signaling Can Lead to Heterologous Desensitization. Cell Signall. 2010 ; 22: 684-696
36. Atwood B. K., Lopez J., Wager-Miller J., Mackie K. A. S.. Expression of G Protein-Coupled Receptors and Related Proteins in HEK293, AtT-20, BV8 and N18 Cell Lines as Revealed by Microarray Analysis. BMC Genomics. 2011 ; 12: 14