R L Papke

Summary

Affiliation: University of Florida
Country: USA

Publications

  1. ncbi request reprint Enhanced inhibition of a mutant neuronal nicotinic acetylcholine receptor by agonists: protection of function by (E)-N-methyl-4-(3-pyridinyl)-3-butene-1-amine (TC-2403)
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
    J Pharmacol Exp Ther 301:765-73. 2002
  2. ncbi request reprint The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville 32610 0267, USA
    Neurosci Lett 256:163-6. 1998
  3. ncbi request reprint Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes
    R L Papke
    Department of Pharmacology, University of Florida, PO Box 100267, 1600 SW Archer Rd, Gainesville, FL 32610, USA
    Bioorg Med Chem Lett 14:1849-53. 2004
  4. pmc Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis
    Roger L Papke
    Department of Pharmacology and Therapeutics, Box 100267 JHMHSC, University of Florida, Gainesville, Florida, FL 32610 0267, USA
    Br J Pharmacol 137:49-61. 2002
  5. ncbi request reprint Inhibition of wild-type and mutant neuronal nicotinic acetylcholine receptors by local anesthetics
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
    Mol Pharmacol 60:1365-74. 2001
  6. ncbi request reprint Analysis of mecamylamine stereoisomers on human nicotinic receptor subtypes
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610, USA
    J Pharmacol Exp Ther 297:646-56. 2001
  7. ncbi request reprint The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida, USA
    J Neurochem 75:204-16. 2000
  8. ncbi request reprint alpha7 receptor-selective agonists and modes of alpha7 receptor activation
    R L Papke
    Department of Pharmacology and Therapeutics, Medical College, University of Florida, Gainesville, FL 32610 0267, USA
    Eur J Pharmacol 393:179-95. 2000
  9. ncbi request reprint alpha7 Nicotinic receptor gene delivery into mouse hippocampal neurons leads to functional receptor expression, improved spatial memory-related performance, and tau hyperphosphorylation
    K Ren
    Department of Pharmaceutics, Box 100494, University of Florida, Gainesville, FL 32610, USA
    Neuroscience 145:314-22. 2007
  10. ncbi request reprint Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors
    Nicole A Horenstein
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610, USA
    J Biol Chem 282:5899-909. 2007

Collaborators

Detail Information

Publications37

  1. ncbi request reprint Enhanced inhibition of a mutant neuronal nicotinic acetylcholine receptor by agonists: protection of function by (E)-N-methyl-4-(3-pyridinyl)-3-butene-1-amine (TC-2403)
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
    J Pharmacol Exp Ther 301:765-73. 2002
    ..The ability of TC-2403 to protect receptor function from agonist-induced inhibition may point toward valuable new combination drug therapies...
  2. ncbi request reprint The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville 32610 0267, USA
    Neurosci Lett 256:163-6. 1998
    ....
  3. ncbi request reprint Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes
    R L Papke
    Department of Pharmacology, University of Florida, PO Box 100267, 1600 SW Archer Rd, Gainesville, FL 32610, USA
    Bioorg Med Chem Lett 14:1849-53. 2004
    ..Thus, AR-R17779 was confirmed to be a selective nicotinic alpha7 receptor agonist and to be without activity at 5HT(3) receptors. In contrast, the actions of tropisetron and ondansetron on nicotinic receptors were complex...
  4. pmc Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis
    Roger L Papke
    Department of Pharmacology and Therapeutics, Box 100267 JHMHSC, University of Florida, Gainesville, Florida, FL 32610 0267, USA
    Br J Pharmacol 137:49-61. 2002
    ..Since these concentrations are relatively non-desensitizing, the contribution of choline-activated alpha7 receptor current may play a significant role in the regulation of calcium homeostasis in alpha7-expressing neurons...
  5. ncbi request reprint Inhibition of wild-type and mutant neuronal nicotinic acetylcholine receptors by local anesthetics
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
    Mol Pharmacol 60:1365-74. 2001
    ....
  6. ncbi request reprint Analysis of mecamylamine stereoisomers on human nicotinic receptor subtypes
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610, USA
    J Pharmacol Exp Ther 297:646-56. 2001
    ..e., therapeutic) application, S-(+)-mecamylamine might be preferable to R-(-)-mecamylamine in terms of equilibrium inactivation of neuronal receptors with decreased side effects associated with muscle-type receptors...
  7. ncbi request reprint The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype
    R L Papke
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida, USA
    J Neurochem 75:204-16. 2000
    ....
  8. ncbi request reprint alpha7 receptor-selective agonists and modes of alpha7 receptor activation
    R L Papke
    Department of Pharmacology and Therapeutics, Medical College, University of Florida, Gainesville, FL 32610 0267, USA
    Eur J Pharmacol 393:179-95. 2000
    ..The data, therefore, suggest that a sufficient level of agonist occupation can be retained on the receptor to promote activation for up to several hundred milliseconds...
  9. ncbi request reprint alpha7 Nicotinic receptor gene delivery into mouse hippocampal neurons leads to functional receptor expression, improved spatial memory-related performance, and tau hyperphosphorylation
    K Ren
    Department of Pharmaceutics, Box 100494, University of Florida, Gainesville, FL 32610, USA
    Neuroscience 145:314-22. 2007
    ....
  10. ncbi request reprint Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors
    Nicole A Horenstein
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610, USA
    J Biol Chem 282:5899-909. 2007
    ....
  11. ncbi request reprint Estimation of both the potency and efficacy of alpha7 nAChR agonists from single-concentration responses
    Roger L Papke
    Pharmacology and Therapeutics 100267 JHMHSC, 1600 SW Archer Rd University of Florida, College of Medicine Gainesville, FL 32610, USA
    Life Sci 78:2812-9. 2006
    ..This extended analysis, combined with automated recording methods, should greatly increase the efficiency with which promising new drug candidates can be characterized...
  12. ncbi request reprint Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytes
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, 32610, USA
    Eur J Pharmacol 524:11-8. 2005
    ..They also point to the potential importance of a newly identified sequence element for modeling the specific amino acids involved with receptor activation...
  13. ncbi request reprint An alpha7 nicotinic acetylcholine receptor gain-of-function mutant that retains pharmacological fidelity
    Andon N Placzek
    Department of Pharmacology and Therapeutics, P O Box 100267, University of Florida, Gainesville, Florida 32610 0267, USA
    Mol Pharmacol 68:1863-76. 2005
    ....
  14. ncbi request reprint The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discovery
    Roger L Papke
    Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, Florida 32610, USA
    J Neurochem 101:160-7. 2007
    ..Thus, understanding the actions of nornicotine in the brain may have significance for both emerging therapeutics and the management of nicotine dependence...
  15. ncbi request reprint Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors
    Fedra M Leonik
    Department of Chemistry, University of Florida, Gainesville, FL 32611 7200, USA
    Bioorg Med Chem Lett 17:1520-2. 2007
    ..Arylidene groups at the 3-position and N-methyl quinuclidine were found to be selective agonists with EC(50)s of 1.5 and 40 microM, respectively...
  16. ncbi request reprint Partial agonist and neuromodulatory activity of S 24795 for alpha7 nAChR responses of hippocampal interneurons
    Gretchen Lopez-Hernandez
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, FL 32610, USA
    Neuropharmacology 53:134-44. 2007
    ..This dilution factor was consistent with the potency of ACh and S 24795 in the oocyte expression system (EC(50)s approximately 30 microM)...
  17. pmc Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: 1-(3-Picolinium)-12-triethylammonium-dodecane dibromide (TMPD)
    Linda P Dwoskin
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536 0082, USA
    Biochem Pharmacol 74:1271-82. 2007
    ....
  18. pmc Modulation of spontaneous hippocampal synaptic events with 5-hydroxyindole, 4OH-GTS-21, and rAAV-mediated alpha7 nicotinic receptor gene transfer
    Jeffrey S Thinschmidt
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610, USA
    Brain Res 1203:51-60. 2008
    ....
  19. pmc PATE gene clusters code for multiple, secreted TFP/Ly-6/uPAR proteins that are expressed in reproductive and neuron-rich tissues and possess neuromodulatory activity
    Fiana Levitin
    Department of Cell Research and Immunology, Tel Aviv University, Ramat Aviv, 69978 Israel
    J Biol Chem 283:16928-39. 2008
    ..Taken together, our findings indicate that in addition to participation of the PATE (Pate)-like genes in functions related to fertility and reproduction, some of them likely act as important modulators of neural transmission...
  20. pmc Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, P O Box 100267, JHMHSC, 1600 SW Archer Road, Gainesville, FL 32610 0267, USA
    Neuropharmacology 54:1189-200. 2008
    ..Our data extend the information available on prototypical nAChR antagonists, and establish the alpha4/6 chimera as a useful new tool for screening drugs as selective nAChR antagonists...
  21. ncbi request reprint In vivo characterization of a novel inhibitor of CNS nicotinic receptors
    M Imad Damaj
    Department Pharmacology and Toxicology, Medical College Virginia Campus, Virginia Commonwealth University, Box 980613, Richmond VA 23298 0613, USA
    Eur J Pharmacol 521:43-8. 2005
    ..These results indicate that TMPH may possess unique selectivity for specific nicotinic receptor subtypes...
  22. pmc The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion
    Roger L Papke
    University of Florida, College of Medicine, 1600 SW Archer Road, Gainesville, FL 32610, USA
    Bioorg Med Chem Lett 15:3874-80. 2005
    ....
  23. pmc Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding
    Xiaoqin Huang
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 725 Rose Street, Lexington, Kentucky 40536, USA
    J Med Chem 51:6293-302. 2008
    ..The new insights into the binding and structure-activity relationship obtained from this study should be valuable for future rational design of more potent and selective agonists of the alpha7 receptor...
  24. ncbi request reprint Activation and inhibition of native neuronal alpha-bungarotoxin-sensitive nicotinic ACh receptors
    Vladimir V Uteshev
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Box 100267 JHMHSC, 1600 SW Archer Rd, University of Florida, Gainesville 32610 0267, FL, USA
    Brain Res 948:33-46. 2002
    ..This could then provide the basis for cytoprotective effects of 4OH-GTS-21 and other nicotinic agonists, mediating trophic and neuromodulatory functions...
  25. ncbi request reprint Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptors
    Vladimir V Uteshev
    Department of Pharmacology and Therapeutics, University of Florida College of Medicine, University of Florida, Gainesville, Florida 32610 0267, USA
    J Neurophysiol 89:1797-806. 2003
    ....
  26. ncbi request reprint Nicotinic receptors on local circuit neurons in dentate gyrus: a potential role in regulation of granule cell excitability
    Charles J Frazier
    Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
    J Neurophysiol 89:3018-28. 2003
    ..Such a relationship between these two afferent pathways could be highly relevant to the study of both age-related memory dysfunction and disorders involving regulation of excitability, such as temporal lobe epilepsy...
  27. ncbi request reprint Hydroxy metabolites of the Alzheimer's drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration
    William R Kem
    Department of Pharmacology and Therapeutics, College of Medicine, University of Florida, Gainesville, FL 32610 0267, USA
    Mol Pharmacol 65:56-67. 2004
    ..Benzylidene anabaseines pharmacologically similar to the hydroxy metabolites, but which enter the brain more readily, may provide greater stimulation of alpha7 receptors in the whole organism...
  28. ncbi request reprint The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase
    Mario B Marrero
    Targacept Inc, 200 East First Street, Suite 300, Winston Salem, NC 27101 4165, USA
    J Pharmacol Exp Ther 309:16-27. 2004
    ..This study supports central and opposite roles for JAK2 and SHP-1 in the control of apoptosis and alpha7-mediated neuroprotection in PC12 cells...
  29. ncbi request reprint Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy
    Roger L Papke
    Department of Pharmacology and Therapeutics, University of Florida, PO Box 100267 JHMHSC, Gainesville, FL 32610 0267, USA
    Neuropharmacology 46:1023-38. 2004
    ....
  30. ncbi request reprint The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors
    Clare Stokes
    Department of Pharmacology and Therapeutics, P O Box 100267, 1600 SW Archer Rd, University of Florida, College of Medicine, Gainesville, FL 32610, USA
    Mol Pharmacol 66:14-24. 2004
    ..Specific features in the agonist molecule itself are also identified that interact with these structural features of the receptor agonist binding site...
  31. ncbi request reprint A single point mutation confers properties of the muscle-type nicotinic acetylcholine receptor to homomeric alpha7 receptors
    Andon N Placzek
    Department of Pharmacology and Therapeutics, J Hills Miller Health Science Center, University of Florida, Gainesville, FL 32610 0267, USA
    Mol Pharmacol 66:169-77. 2004
    ..Thus, the alpha7 TM2 T6'F mutant displays several features that are similar to the muscle nAChR, some of which are not typically thought to be regulated by the pore-lining domain of the receptor...
  32. ncbi request reprint The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker 2,2,6,6-tetramethylpiperidin-4-yl heptanoate
    Roger L Papke
    Department of Pharmacology and Therapeutics, 100267 JHMHSC, College of Medicine, University of Florida, 1600 SW Archer Rd, Gainesville, FL 32610, USA
    Mol Pharmacol 67:1977-90. 2005
    ..Our data indicate great potential utility for TMPH to help relate the diverse central nervous system effects to specific nAChR subtypes...
  33. ncbi request reprint Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist
    Roger L Papke
    University of Florida College of Medicine, Department of Pharmacology and Therapeutics, Gainesville, FL 32610 0267, USA
    Neurosci Lett 378:140-4. 2005
    ....
  34. ncbi request reprint Multiple calcium channels and kinases mediate alpha7 nicotinic receptor neuroprotection in PC12 cells
    Ke Ren
    Department of Pharmaceutics, University of Florida, Gainesville, Florida 32610, USA
    J Neurochem 94:926-33. 2005
    ..ERK1/2 but not JNK and p38 were activated by GTS-21, and the ERK phosphorylation inhibitors PD98059 and U0126 blocked protection...
  35. ncbi request reprint Functional central nicotinic acetylcholine receptor antagonism by systemic administration of Tinuvin 770 (BTMPS)
    John H Graham
    Medical College of Georgia, Alzheimer s Research Center, Augusta, GA 30912 2300, USA
    Curr Alzheimer Res 2:141-7. 2005
    ..Therefore, BTMPS can be considered as an alternative to or as a confirmatory drug for mecamylamine when inhibition of central nicotinic receptors is required...
  36. ncbi request reprint Septal innervation regulates the function of alpha7 nicotinic receptors in CA1 hippocampal interneurons
    Jeffrey S Thinschmidt
    Evelyn F McKnight Brain Institute, Department of Neuroscience, University of Florida, Gainesville, FL 32610, USA
    Exp Neurol 195:342-52. 2005
    ....
  37. ncbi request reprint Medial septal/diagonal band cells express multiple functional nicotinic receptor subtypes that are correlated with firing frequency
    Jeffrey S Thinschmidt
    Evelyn F and William L McKnight Brain Institute, Gainesville, FL 32610, USA
    Neurosci Lett 389:163-8. 2005
    ..Responses to ACh were not affected by tetrodotoxin (TTX) and CdC l(2) but were blocked by MLA or MLA and MEC, suggesting that these currents involve direct activation of nicotinic receptors...