John Traynor

Summary

Affiliation: University of Michigan
Country: USA

Publications

  1. ncbi request reprint Differential binding properties of oripavines at cloned mu- and delta-opioid receptors
    K O Lee
    Department of Pharmacology, University of Michigan, Ann Arbor 48109 0632, USA
    Eur J Pharmacol 378:323-30. 1999
  2. ncbi request reprint Opioid receptor interacting proteins and the control of opioid signaling
    Jennifer T Lamberts
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, 1150 West Medical Center Drive, Ann Arbor, MI 48109 5632, USA
    Curr Pharm Des 19:7333-47. 2013
  3. pmc Modulation of μ-opioid receptor signaling by RGS19 in SH-SY5Y cells
    Qin Wang
    Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109 5632, USA
    Mol Pharmacol 83:512-20. 2013
  4. pmc μ-Opioid receptors and regulators of G protein signaling (RGS) proteins: from a symposium on new concepts in mu-opioid pharmacology
    John Traynor
    Department of Pharmacology and Substance Abuse Research Center, University of Michigan, Ann Arbor, MI 48109 5632, United States
    Drug Alcohol Depend 121:173-80. 2012
  5. doi request reprint Regulator of G protein-signaling proteins and addictive drugs
    John Traynor
    Department of Pharmacology and Substance Abuse Research Center, University of Michigan, Ann Arbor, Michigan 48109 5632, USA
    Ann N Y Acad Sci 1187:341-52. 2010
  6. ncbi request reprint Relationship between rate and extent of G protein activation: comparison between full and partial opioid agonists
    John R Traynor
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 300:157-61. 2002
  7. ncbi request reprint Regulators of G protein signaling & drugs of abuse
    John R Traynor
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
    Mol Interv 5:30-41. 2005
  8. ncbi request reprint Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group
    J R Traynor
    Department of Chemistry, Loughborough University, UK
    J Pharmacol Exp Ther 291:1093-9. 1999
  9. pmc Gi/o-coupled receptors compete for signaling to adenylyl cyclase in SH-SY5Y cells and reduce opioid-mediated cAMP overshoot
    Erica S Levitt
    Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109 5632, USA
    Mol Pharmacol 79:461-71. 2011
  10. pmc Studies of micro-, kappa-, and delta-opioid receptor density and G protein activation in the cortex and thalamus of monkeys
    M C H Ko
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 306:179-86. 2003

Research Grants

  1. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2009
  2. OPIOID RECEPTOR MECHANISMS
    John R Traynor; Fiscal Year: 2010
  3. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2007
  4. Role of Lipid Rafts in Adenylyl Cyclase Sensitization
    John Traynor; Fiscal Year: 2007
  5. POSTDOCTORAL TRAINING IN THE BIOLOGY OF DRUG ABUSE
    John Traynor; Fiscal Year: 2007
  6. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2007
  7. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2006
  8. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2004
  9. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2003
  10. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2002

Collaborators

  • James Woods
  • Mei Chuan Ko
  • HENRY MOSBERG
  • A Coop
  • H T Lee
  • J A Vivian
  • S M Husbands
  • Emily M Jutkiewicz
  • Mario D Aceto
  • Richard Neubig
  • M Spetea
  • Deborah L Heyl
  • PHILIP PORTOGHESE
  • Rae R Matsumoto
  • Roger Sunahara
  • Mary J Clark
  • John W Lewis
  • Daniel C Broom
  • Sanjay K Srivastava
  • M J Przydzial
  • Susan L Mercer
  • M J Clark
  • Kenner C Rice
  • Jennifer T Lamberts
  • Qin Wang
  • A Alt
  • Erica S Levitt
  • Carl N Miller
  • Huailing Zhong
  • M F Divin
  • Hong Xie
  • Mary F Divin
  • Christopher W Cunningham
  • Jun Xu Li
  • David L Roman
  • Veronica Gonzalez-Nunez
  • David Rennison
  • Nick P R Nieland
  • Patrick A Lester
  • I J McFadyen
  • H Houshyar
  • K E Bosse
  • I D Pogozheva
  • Cedric Chauvignac
  • Claire L Neilan
  • Anna Waller
  • Jennifer J Linderman
  • Everette L May
  • C Harrison
  • Elisabeth Greiner
  • Louis S Harris
  • Peter Grundt
  • John E Folk
  • Lauren C Purington
  • F I Carroll
  • F A Bradbury
  • M C Holden Ko
  • Hazem E Hassan
  • K O Lee
  • Natalie D Eddington
  • J J Linderman
  • Jamaluddin Shaikh
  • Jeffery N Talbot
  • Rebecca A Roof
  • Ze Hui Gong
  • Charles P France
  • Ginger L Becker
  • Jillian Broadbear
  • Humphrey A Moynihan
  • Raquel E Rodriguez
  • Humphrey Moynihan
  • Simon Carrington
  • Alejandro Barrallo
  • E Sawyer
  • T A Tharp
  • J C Ho
  • S M Andrews
  • Shefali Shefali
  • Karyn L Sutton
  • Afaf Absood
  • Geneva M Omann
  • Simon Breeden
  • Tamara L Kinzer-Ursem
  • Peter J Woolf
  • Susan M Wade
  • Andrew R Jales
  • Falko Schüllner
  • Roland Krassnig
  • Helmut Schmidhammer
  • Edward R Bowman

Detail Information

Publications56

  1. ncbi request reprint Differential binding properties of oripavines at cloned mu- and delta-opioid receptors
    K O Lee
    Department of Pharmacology, University of Michigan, Ann Arbor 48109 0632, USA
    Eur J Pharmacol 378:323-30. 1999
    ..The ability of oripavine agonists to bind with high affinity to the low agonist affinity state of the nu-opioid receptor may explain the high potencies of these compounds in vivo...
  2. ncbi request reprint Opioid receptor interacting proteins and the control of opioid signaling
    Jennifer T Lamberts
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, 1150 West Medical Center Drive, Ann Arbor, MI 48109 5632, USA
    Curr Pharm Des 19:7333-47. 2013
    ..This review will present current knowledge of such proteins and how they may provide targets for future drug design. ..
  3. pmc Modulation of μ-opioid receptor signaling by RGS19 in SH-SY5Y cells
    Qin Wang
    Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109 5632, USA
    Mol Pharmacol 83:512-20. 2013
    ....
  4. pmc μ-Opioid receptors and regulators of G protein signaling (RGS) proteins: from a symposium on new concepts in mu-opioid pharmacology
    John Traynor
    Department of Pharmacology and Substance Abuse Research Center, University of Michigan, Ann Arbor, MI 48109 5632, United States
    Drug Alcohol Depend 121:173-80. 2012
    ....
  5. doi request reprint Regulator of G protein-signaling proteins and addictive drugs
    John Traynor
    Department of Pharmacology and Substance Abuse Research Center, University of Michigan, Ann Arbor, Michigan 48109 5632, USA
    Ann N Y Acad Sci 1187:341-52. 2010
    ....
  6. ncbi request reprint Relationship between rate and extent of G protein activation: comparison between full and partial opioid agonists
    John R Traynor
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 300:157-61. 2002
    ..The results are consistent with the idea that the active state(s) of the receptor induced by full or partial agonists is the same, but the number of activated receptors determines the rate of G protein activation...
  7. ncbi request reprint Regulators of G protein signaling & drugs of abuse
    John R Traynor
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109, USA
    Mol Interv 5:30-41. 2005
    ..Finally, we consider if RGS proteins represent viable targets for drug abuse medications...
  8. ncbi request reprint Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group
    J R Traynor
    Department of Chemistry, Loughborough University, UK
    J Pharmacol Exp Ther 291:1093-9. 1999
    ..The results show that the configuration of the hydroxyl group is not important in binding affinity at mu-, delta-, or kappa-receptors but does influence kappa-potency and kappa-efficacy, particularly in vivo...
  9. pmc Gi/o-coupled receptors compete for signaling to adenylyl cyclase in SH-SY5Y cells and reduce opioid-mediated cAMP overshoot
    Erica S Levitt
    Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109 5632, USA
    Mol Pharmacol 79:461-71. 2011
    ..These results indicate that multiple receptors could be tethered into complexes with cognate signaling proteins and that access to shared AC by multiple receptor types may provide a means to prevent opioid withdrawal...
  10. pmc Studies of micro-, kappa-, and delta-opioid receptor density and G protein activation in the cortex and thalamus of monkeys
    M C H Ko
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 306:179-86. 2003
    ..In particular, the relative densities of opioid receptor binding sites in the two brain areas reflect their functional roles in the pharmacological actions of opioids in the central nervous system of primates...
  11. ncbi request reprint kappa-Opioid receptor effects of butorphanol in rhesus monkeys
    J A Vivian
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, USA
    J Pharmacol Exp Ther 290:259-65. 1999
    ....
  12. pmc Orphanin FQ inhibits capsaicin-induced thermal nociception in monkeys by activation of peripheral ORL1 receptors
    M C H Ko
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, USA
    Br J Pharmacol 135:943-50. 2002
    ..7. These results provide the first functional evidence that activation of peripheral ORL1 receptors produces thermal antinociception in primates and this action is independent of antinociception produced at classical opioid receptors...
  13. pmc Mu and Delta opioid receptors activate the same G proteins in human neuroblastoma SH-SY5Y cells
    A Alt
    Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    Br J Pharmacol 135:217-25. 2002
    ..5. The findings support the hypothesis that mu- and delta-opioid receptors share a common G protein pool, possibly through a close organization of the two receptors and G protein at the plasma membrane...
  14. ncbi request reprint Stimulation of guanosine-5'-o-(3-[35S]thio)triphosphate binding in digitonin-permeabilized C6 rat glioma cells: evidence for an organized association of mu-opioid receptors and G protein
    A Alt
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan 48109-0632, USA
    J Pharmacol Exp Ther 298:116-21. 2001
    ..A model that assumes an organized association of G proteins with receptors better describes the activation of G proteins by opioid mu-receptors...
  15. ncbi request reprint The steroid 17alpha-acetoxy-6-dimethylaminomethyl-21-fluoro-3-ethoxy-pregna-3, 5-dien-20-one (SC17599) is a selective mu-opioid agonist: implications for the mu-opioid pharmacophore
    I J McFadyen
    Department of Pharmacology, University of Michigan, Ann Arbor, Michigan, USA
    Mol Pharmacol 58:669-76. 2000
    ....
  16. ncbi request reprint Roles of residues 3 and 4 in cyclic tetrapeptide ligand recognition by the kappa-opioid receptor
    M J Przydzial
    Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 65:333-42. 2005
    ..The magnitude of this energy penalty depends on the nature of the fourth residue of the peptide (d-Pen or d-Cys) and correlates well with the observed kappa-receptor binding affinity...
  17. pmc Neutral antagonist activity of naltrexone and 6beta-naltrexol in naïve and opioid-dependent C6 cells expressing a mu-opioid receptor
    M F Divin
    Department of Pharmacology, University of Michigan, 1150 W Medical Center Drive, Ann Arbor, MI 48109 5632, USA
    Br J Pharmacol 156:1044-53. 2009
    ..This hypothesis depends on an accurate characterization of neutral and inverse agonist properties of opioid antagonists...
  18. ncbi request reprint The [35S]GTPgammaS binding assay: approaches and applications in pharmacology
    C Harrison
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, West Medical Center Drive, Ann Arbor, MI 48109 0632, USA
    Life Sci 74:489-508. 2003
    ....
  19. ncbi request reprint Antinociceptive and other behavioral effects of the steroid SC17599 are mediated by the mu-opioid receptor
    H Houshyar
    Department of Pharmacology, University of Michigan, Ann Arbor, MI 48109, USA
    Eur J Pharmacol 395:121-8. 2000
    ..The steroid SC17599 is structurally a very unusually selective mu-opioid agonist that produces behavioral effects, which are similar, but not identical, to those of morphine...
  20. ncbi request reprint Design of high affinity cyclic pentapeptide ligands for kappa-opioid receptors
    M J Przydzial
    Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA
    J Pept Res 66:255-62. 2005
    ..Nonetheless, the high affinity KOR peptides in this series represent excellent leads for the development of structurally related, selective KOR ligands designed to exploit structurally specific features of KOR, MOR, and DOR...
  21. doi request reprint Endogenous regulators of G protein signaling differentially modulate full and partial mu-opioid agonists at adenylyl cyclase as predicted by a collision coupling model
    M J Clark
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, USA
    Mol Pharmacol 73:1538-48. 2008
    ....
  22. ncbi request reprint Characterization of opioid-binding sites in zebrafish brain
    Veronica Gonzalez-Nunez
    Department of Biochemistry and Molecular Biology, Faculty of Medicine, University of Salamanca, Spain
    J Pharmacol Exp Ther 316:900-4. 2006
    ..Hence, the study of zebrafish opioid activity may contribute to an understanding of endogenous opioid systems in higher vertebrates...
  23. pmc Differential behavioral tolerance to the delta-opioid agonist SNC80 ([(+)-4-[(alphaR)-alpha-[(2S,5R)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-methoxyphenyl)methyl]-N,N-diethylbenzamide) in Sprague-Dawley rats
    Emily M Jutkiewicz
    1301 MSRB III, Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 315:414-22. 2005
    ..Overall, the lack of observable tolerance to the antidepressant-like effects of SNC80 indicates that this class of compounds has potential as a novel antidepressant therapy...
  24. pmc Differential in vivo potencies of naltrexone and 6beta-naltrexol in the monkey
    M C Holden Ko
    Department of Pharmacology, University of Michigan, Ann Arbor, 48109 0632, USA
    J Pharmacol Exp Ther 316:772-9. 2006
    ....
  25. ncbi request reprint Comparison of the in vitro efficacy of mu, delta, kappa and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes
    Patrick A Lester
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    Brain Res 1073:290-6. 2006
    ..The results show that the ability of agonists to stimulate [35S]GTPgammaS binding relates to the receptor distribution of opioid and ORL1 receptors in the dog...
  26. ncbi request reprint Thienorphine: receptor binding and behavioral effects in rhesus monkeys
    Jun Xu Li
    Department of Pharmacology, The University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Dr, Mail Code 7792, San Antonio, TX 78229 3900, USA
    J Pharmacol Exp Ther 321:227-36. 2007
    ..Thienorphine and U50,488 produced the same directly observable signs. These results show that thienorphine has long-lasting effects that seem to be mediated by low-efficacy agonism at kappa-opioid receptors, both in vitro and in vivo...
  27. pmc Comparison of the opioid receptor antagonist properties of naltrexone and 6 beta-naltrexol in morphine-naïve and morphine-dependent mice
    Mary F Divin
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 5632, USA
    Eur J Pharmacol 583:48-55. 2008
    ....
  28. pmc Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs
    Christopher W Cunningham
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA
    J Med Chem 51:2316-20. 2008
    ..Additionally, 7 demonstrated morphine-like antinociceptive potency in mice, indicating this compound as an ideal lead to further evaluate the role of P-gp in opioid analgesic tolerance development...
  29. pmc Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring
    David Rennison
    University of Bristol, Cantock s Close, Bristol, BS8 1TS, United Kingdom
    J Med Chem 49:6104-10. 2006
    ..Wash-resistant binding was observed within this series and appeared to be unrelated to side-chain length...
  30. pmc The spinal antinociceptive effects of endomorphins in rats: behavioral and G protein functional studies
    Hong Xie
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    Anesth Analg 106:1873-81. 2008
    ..t.) administration of endomorphin-1 and -2 on nociception assays and G protein activation with those of [d-Ala(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin (DAMGO), a highly effective peptidic mu-opioid receptor agonist...
  31. ncbi request reprint BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism
    Stephen M Husbands
    Department of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK
    Eur J Pharmacol 509:117-25. 2005
    ..The slow onset, long-duration kappa opioid receptor agonist effects of BU74 suggests that it could be a lead compound for the discovery of a treatment for cocaine abuse...
  32. ncbi request reprint Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan
    Sanjay K Srivastava
    Department of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, U K
    J Med Chem 47:6645-8. 2004
    ..The TOMI derivatives (8) were DOR agonists with significant selectivity. In vivo the DOR antagonist activity of 7d was confirmed, but the predominant agonist effect of 8d was shown to be mu opioid receptor mediated...
  33. ncbi request reprint Nonpeptidic delta-opioid receptor agonists reduce immobility in the forced swim assay in rats
    Daniel C Broom
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    Neuropsychopharmacology 26:744-55. 2002
    ..Thus, delta-agonists differ from typical antidepressants in the forced swim assay...
  34. ncbi request reprint Convulsant activity of a non-peptidic delta-opioid receptor agonist is not required for its antidepressant-like effects in Sprague-Dawley rats
    Daniel C Broom
    Department of Pharmacology, University of Michigan Medical School, 1301 Medical Science Research Building III, Ann Arbor, MI 48109 0632, USA
    Psychopharmacology (Berl) 164:42-8. 2002
    ..Non-peptidic delta-opioid receptor agonists possess antidepressant-like activity in the forced swim assay in the rat. These compounds have also previously been shown to possess convulsant properties in mice...
  35. ncbi request reprint Comparison of receptor mechanisms and efficacy requirements for delta-agonist-induced convulsive activity and antinociception in mice
    Daniel C Broom
    Department of Pharmacology, University of Michigan Medical School, 1150 West Medical Center Drive, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 303:723-9. 2002
    ....
  36. ncbi request reprint Behavioral effects of delta-opioid receptor agonists: potential antidepressants?
    Daniel C Broom
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor 48109 0632, USA
    Jpn J Pharmacol 90:1-6. 2002
    ..These studies propose that the delta-opioid receptor may provide a new therapeutic target for treating human depression...
  37. ncbi request reprint Endogenous RGS protein action modulates mu-opioid signaling through Galphao. Effects on adenylyl cyclase, extracellular signal-regulated kinases, and intracellular calcium pathways
    Mary J Clark
    Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    J Biol Chem 278:9418-25. 2003
    ....
  38. ncbi request reprint Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships
    Elisabeth Greiner
    Department of Pharmaceutical Chemistry, Institute of Pharmacy, University of Innsbruck, Innrain 52a, A 6020 Innsbruck, Austria
    J Med Chem 46:1758-63. 2003
    ..09 nm)...
  39. ncbi request reprint 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity
    Sanjay K Srivastava
    School of Chemistry, University of Bristol, Bristol BS8 1TS, UK
    J Med Chem 45:537-40. 2002
    ..In mice in vivo assays 5a showed good delta antagonist activity in the anti-writhing analgesic assay and also inhibited delta agonist-induced convulsant activity...
  40. ncbi request reprint Delta-opioid agonists: differential efficacy and potency of SNC80, its 3-OH (SNC86) and 3-desoxy (SNC162) derivatives in Sprague-Dawley rats
    Emily M Jutkiewicz
    Department of Pharmacology 1301 MSRB 3, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 309:173-81. 2004
    ....
  41. ncbi request reprint Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist
    Claire L Neilan
    Department of Pharmacology, University of Michigan, 1301 Medical Science Res Bldg III, Ann Arbor, MI 48109, USA
    Eur J Pharmacol 499:107-16. 2004
    ..BU72 is too efficacious for human use but manipulation to reduce efficacy could provide a lead to the development of a treatment for opioid dependence...
  42. ncbi request reprint Endogenous regulator of G protein signaling proteins suppress Galphao-dependent, mu-opioid agonist-mediated adenylyl cyclase supersensitization
    Mary J Clark
    Department of Pharmacology, University of Michigan Medical Center, Ann Arbor, Michigan 48109 0632, USA
    J Pharmacol Exp Ther 310:215-22. 2004
    ..These results demonstrate a role for Galphao in adenylyl cyclase supersensitization after mu-agonist exposure and show that this action is modulated by endogenous RGS proteins...
  43. ncbi request reprint Receptor binding kinetics and cellular responses of six N-formyl peptide agonists in human neutrophils
    Anna Waller
    Department of Chemical Engineering, University of Michigan, Ann Arbor, Michigan 48105, USA
    Biochemistry 43:8204-16. 2004
    ..However, the interconverting two-receptor state model was not sufficient to predict response potency, suggesting the presence of receptor states not discriminated by the binding data...
  44. pmc Separation of the convulsions and antidepressant-like effects produced by the delta-opioid agonist SNC80 in rats
    Emily M Jutkiewicz
    Department of Pharmacology, University of Michigan Medical School, 1301 MSRB III, Ann Arbor, MI 48109 0632, USA
    Psychopharmacology (Berl) 182:588-96. 2005
    ..Therefore, determining how to separate the convulsive and antidepressant-like characteristics of these compounds is essential for their potential clinical use...
  45. ncbi request reprint Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist
    Cedric Chauvignac
    Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
    J Med Chem 48:1676-9. 2005
    ....
  46. ncbi request reprint Endogenous regulator of g protein signaling proteins reduce {mu}-opioid receptor desensitization and down-regulation and adenylyl cyclase tolerance in C6 cells
    Mary J Clark
    Department of Pharmacology, University of Michigan Medical School, 1301 Medical Science Research Building III, 1150 West Medical Center Drive, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 312:809-15. 2005
    ..The results show that RGS proteins endogenously expressed in C6 cells reduce agonist-induced mu-opioid receptor desensitization, down-regulation, and sensitivity to tolerance to inhibit adenylyl cyclase activity...
  47. pmc Comparison of peptidic and nonpeptidic delta-opioid agonists on guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding in brain slices from Sprague-Dawley rats
    Emily M Jutkiewicz
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    J Pharmacol Exp Ther 312:1314-20. 2005
    ..Finally, these data also revealed that [(35)S]GTPgammaS autoradiography could be used to compare efficacy differences among agonists across various brain regions in rat brain slices...
  48. ncbi request reprint A spatial focusing model for G protein signals. Regulator of G protein signaling (RGS) protien-mediated kinetic scaffolding
    Huailing Zhong
    Department of Pharmacology, The University of Michigan, Ann Arbor, Michigan 48109 0632, USA
    J Biol Chem 278:7278-84. 2003
    ....
  49. ncbi request reprint N-(trifluoromethyl)benzyl substituted N-normetazocines and N-norketobemidones
    Everette L May
    Department of Pharmacology, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298, USA
    Bioorg Med Chem 11:31-3. 2003
    ..In functional in vitro assays, this compound was a weak antagonists, but in apparent contradiction it was inactive in in vivo assays...
  50. pmc Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones
    Nick P R Nieland
    School of Chemistry, University of Bristol, Bristol, BS8 1TS, UK
    J Med Chem 49:5333-8. 2006
    ..The new series also followed the well-established SAR that 17-methyl ligands have greater efficacy at the mu opioid receptor than their 17-cyclopropylmethyl counterparts...
  51. ncbi request reprint 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles
    Peter Grundt
    Department of Pharmacy and Pharmacology, University of Bath, UK
    J Med Chem 46:1563-6. 2003
    ....
  52. ncbi request reprint Assays for G-protein-coupled receptor signaling using RGS-insensitive Galpha subunits
    Mary J Clark
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor 48109 0632, USA
    Methods Enzymol 389:155-69. 2004
    ..The altered signaling in cells expressing RGS-insensitive Galpha(o) subunits allows for determination of the role of endogenous RGS proteins to limit and/or direct signaling...
  53. pmc Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands
    Susan L Mercer
    Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA
    Eur J Med Chem 43:1304-8. 2008
    ..The N-isobutyl, N-phenylpropyl, and N-benzyl analogs are worth pursuing due to their good affinity and selectivity at the sigma(1) receptor, whereas the N-benzyl analog exhibits the greatest selectivity for sigma(1)...
  54. ncbi request reprint Mediation of adenylyl cyclase sensitization by PTX-insensitive GalphaoA, Galphai1, Galphai2 or Galphai3
    Mary J Clark
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan USA
    J Neurochem 99:1494-504. 2006
    ..This serum-mediated sensitization partially masked mu-opioid-mediated sensitization when expressed as percentage overshoot due to an apparent increase in AC activity...
  55. ncbi request reprint Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay
    David L Roman
    Department of Pharmacology, University of Michigan Medical School, 1150 W Medical Center Drive, 1303 MSRB III, Ann Arbor, MI 41809, USA
    Mol Pharmacol 71:169-75. 2007
    ..Thus, we demonstrate the feasibility of targeting RGS/Galpha protein-protein interactions with small molecules as a novel means to modulate GPCR-mediated signaling processes...
  56. ncbi request reprint pKa and volume of residue one influence delta/mu opioid binding: QSAR analysis of tyrosine replacement in a nonselective deltorphin analogue
    Deborah L Heyl
    Department of Chemistry, Eastern Michigan University, Ypsilanti, MI 48197, USA
    Bioorg Med Chem 11:3761-8. 2003
    ..The pK(a) effect is stronger on delta than on mu binding, generating an increase in delta selectivity with increasing residue-one pK(a)...

Research Grants15

  1. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2009
    ..An understanding of roles for RGS proteins in the actions of mu-opioids may lead to improvements in the treatment of pain as well as treatment of opioid and stimulant abuse. ..
  2. OPIOID RECEPTOR MECHANISMS
    John R Traynor; Fiscal Year: 2010
    ..An understanding of roles for RGS proteins in the actions of mu-opioids may lead to improvements in the treatment of pain as well as treatment of opioid and stimulant abuse. ..
  3. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2007
    ..An understanding of roles for RGS proteins in the actions of mu-opioids may lead to improvements in the treatment of pain as well as treatment of opioid and stimulant abuse. ..
  4. Role of Lipid Rafts in Adenylyl Cyclase Sensitization
    John Traynor; Fiscal Year: 2007
    ....
  5. POSTDOCTORAL TRAINING IN THE BIOLOGY OF DRUG ABUSE
    John Traynor; Fiscal Year: 2007
    ..They include state-of-the-art tools for mouse and rat genetics, genomics, proteomics, and informatics. Thus, our trainees will profit from a highly sophisticated, yet supportive, research and training environment. ..
  6. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2007
    ..An understanding of roles for RGS proteins in the actions of mu-opioids may lead to improvements in the treatment of pain as well as treatment of opioid and stimulant abuse. ..
  7. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2006
    ..An understanding of roles for RGS proteins in the actions of mu-opioids may lead to improvements in the treatment of pain as well as treatment of opioid and stimulant abuse. ..
  8. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2004
    ..The work will further define opioid signaling and suggest novel therapeutic targets for the treatment of pain and opiate drug abuse. ..
  9. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2003
    ..The work will further define opioid signaling and suggest novel therapeutic targets for the treatment of pain and opiate drug abuse. ..
  10. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2002
    ..The work will further define opioid signaling and suggest novel therapeutic targets for the treatment of pain and opiate drug abuse. ..
  11. OPIOID RECEPTOR MECHANISMS
    John Traynor; Fiscal Year: 2001
    ..The work will further define opioid signaling and suggest novel therapeutic targets for the treatment of pain and opiate drug abuse. ..