Research Topics
Species | Roger PapkeSummaryAffiliation: University of Florida Country: USA Publications
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Publications
The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discoveryRoger 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...- The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker 2,2,6,6-tetramethylpiperidin-4-yl heptanoateRoger 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... - Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonistRoger L Papke
University of Florida College of Medicine, Department of Pharmacology and Therapeutics, Gainesville, FL 32610 0267, USA
Neurosci Lett 378:140-4. 2005.... - Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotineRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, FL 32610 0267, USA
J Pharmacol Exp Ther 329:791-807. 2009.... - High throughput electrophysiology with Xenopus oocytesRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida, USA
Comb Chem High Throughput Screen 12:38-50. 2009..We show some types of data that have been gathered by this system and review realized and potential applications... - The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusionRoger L Papke
University of Florida, College of Medicine, 1600 SW Archer Road, Gainesville, FL 32610, USA
Bioorg Med Chem Lett 15:3874-80. 2005.... - Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimerasRoger 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... - Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytesRoger 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... - Estimation of both the potency and efficacy of alpha7 nAChR agonists from single-concentration responsesRoger 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... - Investigation of the Molecular Mechanism of the ?7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator PNU-120596 Provides Evidence for Two Distinct Desensitized StatesDustin K Williams
Department of Pharmacology and Therapeutics, University of Florida, P O Box 100267, Gainesville, FL 32610 0267
Mol Pharmacol 80:1013-32. 2011..In the presence of high agonist concentrations, competitive antagonists may have the effect of shifting the balance in favor of D(s) and increasing ion channel currents... - Tricks of perspective: insights and limitations to the study of macroscopic currents for the analysis of nAChR activation and desensitizationRoger L Papke
Department of Pharmacology and Therapeutics, College of Medicine, University of Florida, Gainesville, FL 32610 0267, USA
J Mol Neurosci 40:77-86. 2010..In contrast, with an agonist pulse like that used in Xenopus oocyte experiments, microscopic desensitization rates have a profound impact on peak current amplitude and very little effect on the kinetics of the macroscopic responses... - Working with OpusXpress: methods for high volume oocyte experimentsRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, FL 32610, USA
Methods 51:121-33. 2010..Some of our advice is specific to researchers fortunate enough to have access to an OpusXpress system, but most of it is applicable to any group using Xenopus oocytes for the heterologous expression of ion channels... - Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacyRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida, PO Box 100267 JHMHSC, Gainesville, FL 32610 0267, USA
Neuropharmacology 46:1023-38. 2004.... - alpha4beta2 Nicotinic acetylcholine receptors, willing if ableRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida, Gainesville, FL 32610 0267, USA
Br J Pharmacol 160:1903-5. 2010..These observations provide important and intriguing new pieces of the brain nicotine receptor puzzle... - Cysteine accessibility analysis of the human alpha7 nicotinic acetylcholine receptor ligand-binding domain identifies L119 as a gatekeeperRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, FL 32610, USA
Neuropharmacology 60:159-71. 2011..Reaction of L119C with small non-polar reagents increases activation by small agonists but can block the access of large ligands such as benzylidene anabaseines to the ligand-binding domain... - Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytesRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610 0267, USA
J Pharmacol Exp Ther 333:501-18. 2010..Hexamethonium was a relatively nonselective antagonist with mixed competitive and noncompetitive activity... - Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonistsRoger L Papke
Department of Pharmacology and Therapeutics, University of Florida, P O Box 100267, Gainesville, FL 32610 0267, USA
J Pharmacol Exp Ther 337:367-79. 2011..These data indicate the dual effects expected for ?4?2* partial agonists and provide models and insights for utility of partial agonists in therapeutic development... - Partial agonist and neuromodulatory activity of S 24795 for alpha7 nAChR responses of hippocampal interneuronsGretchen 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)... - Septal innervation regulates the function of alpha7 nicotinic receptors in CA1 hippocampal interneuronsJeffrey S Thinschmidt
Evelyn F. McKnight Brain Institute, Department of Neuroscience, University of Florida, Gainesville, FL 32610, USA
Exp Neurol 195:342-52. 2005.... - Modulation of inhibitory synaptic activity by a non-alpha4beta2, non-alpha7 subtype of nicotinic receptors in the substantia gelatinosa of adult rat spinal cordDaisuke Takeda
Department of Oral Surgery, College of Dentistry, University of Florida, 1600 SW Archer Road, Gainesville, FL 32610, USA
Pain 101:13-23. 2003.... - Activation and inhibition of native neuronal alpha-bungarotoxin-sensitive nicotinic ACh receptorsVladimir 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... - Modulation of spontaneous hippocampal synaptic events with 5-hydroxyindole, 4OH-GTS-21, and rAAV-mediated alpha7 nicotinic receptor gene transferJeffrey S Thinschmidt
Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610, USA
Brain Res 1203:51-60. 2008.... - Nicotinic receptors on local circuit neurons in dentate gyrus: a potential role in regulation of granule cell excitabilityCharles 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... - Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptorsNicole A Horenstein
Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610 0267, USA
Mol Pharmacol 74:1496-511. 2008..Our results provide insight for the further development of nicotinic therapeutics and will be useful to direct future experiments with protein structure-based modeling and site-directed mutagenesis... - Tethered agonist analogs as site-specific probes for domains of the human ?7 nicotinic acetylcholine receptor that differentially regulate activation and desensitizationJingyi Wang
Department of Pharmacology and Therapeutics University of Florida, Gainesville, FL 32610 0267, USA
Mol Pharmacol 78:1012-25. 2010..This insight may provide a new approach for drug development... - A single point mutation confers properties of the muscle-type nicotinic acetylcholine receptor to homomeric alpha7 receptorsAndon 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... - Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptorsNicole A Horenstein
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610, USA
J Biol Chem 282:5899-909. 2007.... - An alpha7 nicotinic acetylcholine receptor gain-of-function mutant that retains pharmacological fidelityAndon 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.... - The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptorsClare 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... - Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptorsVladimir 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.... - Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptorsFedra 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... - Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding siteDustin K Williams
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, P O Box 100267, Gainesville, FL 32610 0267, USA
J Pharmacol Exp Ther 330:40-53. 2009.... - Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysisRoger 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... - 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 penetrationWilliam 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... - Positive modulation of alpha7 nAChR responses in rat hippocampal interneurons to full agonists and the alpha7-selective partial agonists, 4OH-GTS-21 and S 24795Gretchen Y López-Hernández
Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, Gainesville, FL 32610 0267, USA
Neuropharmacology 56:821-30. 2009..We demonstrated that the potentiation of alpha7 nAChR response would depend on the nature and the effective concentration of the agonist involved and its particular interaction with the positive modulator... - 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... - Selective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonistsGretchen Y López-Hernández
Department of Pharmacology and Therapeutics, University of Florida, P O Box 100267, Gainesville, FL 32610 0267, USA
Mol Pharmacol 76:652-66. 2009..These agents might be helpful in elucidating complex receptor responses in brain regions with mixed populations of nAChRs... - Multiple calcium channels and kinases mediate alpha7 nicotinic receptor neuroprotection in PC12 cellsKe 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... - Synthesis of H-bonding probes of alpha7 nAChR agonist selectivityJingyi Wang
Department of Chemistry, University of Florida, PO Box 117200, Gainesville, FL 32611 7200, USA
Bioorg Med Chem Lett 19:474-6. 2009..The pyrrole compounds were confirmed to be alpha7 selective, displaying preference for this receptor over muscle and heteromeric neuronal receptor subtypes... - Medial septal/diagonal band cells express multiple functional nicotinic receptor subtypes that are correlated with firing frequencyJeffrey 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... - Taurine-induced long-lasting potentiation in the rat hippocampus shows a partial dissociation from total hippocampal taurine content and independence from activation of known taurine transportersJohn Dominy
Department of Pharmacodynamics, University of Florida College of Pharmacy, Gainesville, FL 32610, USA
J Neurochem 89:1195-205. 2004.... - PATE gene clusters code for multiple, secreted TFP/Ly-6/uPAR proteins that are expressed in reproductive and neuron-rich tissues and possess neuromodulatory activityFiana 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... - Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist bindingXiaoqin 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... - 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.... - 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 phosphataseMario 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... - 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... - In vivo characterization of a novel inhibitor of CNS nicotinic receptorsM 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...
Research Grants
- TARGETING ALPHA7 NACHR FOR THERAPEUTICS EFFECTSRoger Papke; Fiscal Year: 2003..abstract_text> ..
- Targeting alpha7 nAChR for Therapeutic EffectsRoger Papke; Fiscal Year: 2007....
- Targeting alpha7 nAChR for Therapeutic EffectsRoger L Papke; Fiscal Year: 2010....