Selected Reprints in PDF Format
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- Papke, R. L., J. S. Thinschmidt, B. A. Moulton, E. M. Meyer, and A. Poirier. Activation and inhibition of rat neuronal nicotinic receptors by ABT-418. British Journal of Pharmacology 120:429-438 (1997).
- Kem, W. R., V. M. Mahnir, R. L. Papke, and C. J. Lingle. Anabaseine is a potent agonist upon muscle and neuronal alpha-bungarotoxin sensitive nicotinic receptors. Journal of Pharmacology and experimental Therapeutics 283:979-992 (1997).
- Francis, M. M., K. I. Choi, B. A. Horenstein, and R. L. Papke. Sensitivity to voltage-independent inhibition determined by pore-lining region of ACh receptor. Biophysical Journal 74(5):2306-2317 (1998).
- Meyer, E. M., E. T. Tay, J. A. Zoltewicz, R. L. Papke, C. Meyers, M. King, and C. M. d. Fiebre. Neuroprotective and memory-related actions of novel alpha 7 nicotinic agents with different mixed agonist/antagonist properties. Journal of Pharmacology and Experimental Therapeutics 284:1026-1032 (1998).
- Kabakov, A. Y., N. B. Karkanias, R. H. Lenox, and R. L. Papke. Synapse-specific accumulation of lithium in intracellular microdomains: a model for uncoupling coincidence detection in the brain. 28(4):271-279 (1998).
- Papke, R. L., and J. S. Thinschmidt. The Correction of Alpha7 Nicotinic Acetylcholine Receptor Concentration-Response Relationships in Xenopus Oocytes. Neuroscience Letters 256:163-166 (1998).
- Meyer, E., A. Kuryatov, V. Gerzanich, J. Lindstrom, and R. L. Papke. Analysis of 40H-GTS-21 Selectivity and Activity at Human and Rat alpha 7 Nicotinic Receptors. Journal of Pharmacology and Experimental Therapeutics 287(3):918-25 (1998).
- Karkanias, N., and R. Papke. Subtype-specific effects of lithium on glutamate receptor function. 81(4):1506-12 (1999).
- Webster, J. C., M. M. Francis, J. K. Porter, G. Robinson, C. Stokes, B. Horenstein, and R. L. Papke. Antagonist activities of mecamylamine and nicotine show reciprocal dependence on beta subunit sequence in the second transmembrane domain. British Journal of Pharmacology 127:1337-48 (1999).
- Papke, R. L., J. C. Webster, P. M. Lippiello, M. Bencherif, and M. M. Francis. The activation and inhibition of human nAChR by RJR-2403 indicate a selectivity for the a4b2 receptor subtype. Journal of Neurochemistry 75:204-216 (2000).
- Francis, M. M., R. W. Vazquez, R. L. Papke, and R. E. Oswald. Subtype-selective inhibition of neuronal nicotinic acetylcholine receptors by cocaine is determined by the alpha4 and beta4 subunits. Molecular Pharmacology 58(1):109-19 (2000).
- Roger L. Papke, Paul R. Sanberg, R. Douglas Shytle, 2001. Analysis of Mecamylamine Stereoisomers on Human Nicotinic Receptor Subtypes. Journal of Pharmacology and Experimental Therapeutics, 297:646–656,.
- Roger L. Papke, Benjamin A. Horenstein, and Andon N. Placzek. Inhibition of Wild-Type and Mutant Neuronal Nicotinic Acetylcholine Receptors by Local Anesthetics. Molecular Pharmacology. 60:1365–1374, 2001.
- A.Y. Kabakov, Ph.D. and R.L. Papke, Ph.D. Ultra Fast Solution Applications for Prolonged Gap-free Recordings: Controlling a Burleigh Piezo-Electric Positioner with Clampex 7.
- Roger L. Papke 2002. Enhanced inhibition of a mutant neuronal nAChR by
agonists: protection of function by TC-2403. Journal of Pharmacology and
Experimental Therapeutics.301:765-773, 2002.
- Roger L. Papke and Julia K. Porter Papke. Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis. British Journal of Pharmacology,137:49-61, 2002.
- The Use of Net Charge Analysis in the Study of Ion Channel Pharmacology. Axobits, 6-9, 2002.
- The Use of Net Charge Analysis in the Study of Ion Channel Pharmacology- long version.
- Charles J. Frazier, Ben W. Strowbridge, and Roger L. Papke. Nicotinic acetylcholine receptors on local circuit neurons in the dentate gyrus: a potential role in the regulation of granule cell excitability. J Neurophysiol, 89: 3018-3028, 2003.
- William R. Kem, Vladimir M. Mahnir,1 Laszlo Prokai, Roger L. Papke, Xuefang Cao,
Susan LeFrancois, Kristin Wildeboer, Katalin Prokai-Tatrai, Julia Porter-Papke, and Ferenc Soti. 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. Mol Pharmacol,65: 56-67, 2004
- Mario B. Marrero, Roger L. Papke, Balwinder S. Bhatti, Seán Shaw,
and Merouane Bencherif. THE NEUROPROTECTIVE EFFECT OF TC-1698, A NOVEL ALPHA7 LIGAND, IS
PREVENTED THROUGH ANGIOTENSIN II ACTIVATION OF A TYROSINE
PHOSPHATASE. JPET ,309: 16-27 2003
- Clare Stokes, Julia Kay Porter Papke, Nicole A. Horenstein, William R. Kem, Thomas J. McCormack and Roger L. Papke. The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors. Molecular Pharmacology, 66: 14-24, 2004
- John Dominy, Jr., Jeffrey S. Thinschmidt, Joanna Peris, Ralph Dawson, Jr., and
Roger L. Papke. 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 transportersJournal of Neurochemistry, 89: 1195-1205 2004
- Andon N. Placzek, Francesca Grassi, Thaddeus Papke, Edwin M. Meyer, and Roger L. Papke. 2004. A single point mutation confers properties of the muscle-type nicotinic acetylcholine receptor to homomeric alpha7 receptors. Molecular Pharmacology, 66: 169-177, 2004
- Roger L. Papke, Joshua D. Buhr, Michael M. Francis, Kyung Il Choi, Jeffrey S. Thinschmidt, and Nicole A. Horenstein. The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker TMPH. Molecular Pharmacology, 67: 1977-90 2005
- Roger L. Papke, Guangrong Zheng, Nicole A. Horenstein, Linda P. Dwoskin, and Peter A. Crooks. The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion. Bioorganic & Medicinal Chemistry Letters, 15:3874-3880 2005
- Andon N. Placzek, Francesca Grassi, Edwin M. Meyer, and Roger L. Papke. 2005. An alpha7 nicotinic acetylcholine receptor
gain-of-function mutant that retains pharmacological fidelity.Molecular Pharmacology68: 1863-76, 2005
- Nicole A. Horenstein, Thomas J. McCormack, Clare Stokes, Ke Ren, and Roger L. Papke 2006. Reversal of Agonist Selectivity by Mutations of Conserved Amino Acids in the Binding Site of Nicotinic Acetylcholine Receptors.Journal of Biological Chemistry 282: 5899-909
- Fedra M. Leonik, Roger L. Papke, Nicole A. Horenstein. 2007. Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.Bioorganic & Medicinal Chemistry Letters: 17: 1520-22
- Linda P. Dwoskin, Barry M. Joyce, Guangrong Zheng, Nichole M. Neugebauer, Vamshi K. Manda, Paul Lockman, Roger L. Papke, Michael T. Bardo, and Peter A. Crooks. 2007. Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: TMPD.Biochemical Pharmacology 74: 1271-82
- Shafiqur Rahman1, Zhenfa Zhang, Roger L. Papke, Peter A. Crooks, Linda P. Dwoskin, and
Michael T. Bardo. 2008. Region-specific effects of bPiDDB on in vivo nicotine-induced increase in extracellular dopamine.British Journal of Pharmacology153(4):792-804
- Roger L. Papke and Cathy Smith-Maxwell. 2008. High-throughput electrophysiology with Xenopus oocytes.Combinatorial Chemistry and High Throughput Screening12(1):38-50
- Jeffrey S. Thinschmidt, Ke Ren, Michael A. King, Edwin M. Meyer, and Roger L. Papke. 2008. Modulation of spontaneous hippocampal synaptic events with 5-hydroxyindole, 4OH GTS-21, and rAAV- mediated alpha7 nicotinic receptor gene transfer.Brain Research1203:51-60.
- Roger L. Papke, Linda P. Dwoskin, Peter A. Crooks, Guangrong Zheng, Zhenfa Zhang, J. Michael McIntosh and Clare Stokes. 2008. Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras. Neuropharmacology54(8)
1189-200
- Fiana Levitin, Mordechai Weiss, Yoonsoo Hahn, Omer Stern, Roger L. Papke, Robert Matusik, Srinivas R. Nandana, Ravit Ziv, Edward Pichinuk, Sharbel Salame, Tapan Bera, James Vincent, Byungkook Lee, Ira Pastan, and Daniel H. Wreschner. 2008. Gene Clusters Code for Multiple, Secreted, TFP/Ly-6/uPAR Proteins That Are Expressed in Reproductive and Neural-Rich Tissues and Possess Neuromodulatory Activity.Journal of Biological Chemistry283(24)
16928-39
- Nicole A. Horenstein, Fedra M. Leonik, and Roger L. Papke. 2008. Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors.Molecular Pharmacology741496-1511
- Xiaoqin Huang, Fang Zheng, Clare Stokes, Roger L. Papke, and Chang-Guo Zhan. 2008. Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.Journal of Medicinal Chemistry51(20):6293-302
- Gretchen Y. Lopez-Hernandez, Jeffrey S. Thinschmidt, Philippe Morain, Caryn Trocme-Thibierge, William R. Kem, Ferenc Soti, and Roger L. Papke 2009. Positive modulation of alpha7 nAChR responses in rat hippocampal interneurons to full agonists and the alpha7-selective partial agonists, 4OH-GTS-21 and S 24795.Neuropharmacology52:821-830
- Yann S. Mineur, Christoph Eibl, Grace Young, Christopher Kochevar, Roger L. Papke, Daniela Gundisch, Marina R. Picciotto 2009. Cytisine-based nicotinic partial agonists as novel antidepressant compounds.Journal of Pharmacology and Experimental Therapeutics 329:377-86
- Roger L. Papke, William R. Kem, Ferenc Soti, Gretchen Y. Lopez-Hernandez, and Nicole A. Horenstein. 2009. Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine.Journal of Pharmacology and Experimental Therapeutics 329:791-807
- Dustin K. Williams, Clare Stokes, Nicole A. Horenstein, and Roger L. Papke 2009. Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site.Journal of Pharmacology and Experimental Therapeutics330:40-53
- Vladimir P. Grinevich, Roger L. Papke, Patrick M. Lippiello and Merouane Bencherif 2009. Atypical Antipsychotics as Noncompetitive Inhibitors of alpha4beta2 and alpha7 Neuronal Nicotinic Receptors.Neuropharmacology57:183-91
- Roger L. Papke 2009. Tricks of Perspective: Insights and limitations to the study of macroscopic currents for the analysis of nAChR activation and desensitization.Molecular Neuroscience40:77-86
- Gretchen Y. Lopez-Hernandez, Jeffrey S. Thinschmidt, Guangrong Zheng, Zhenfa Zhang, Peter A. Crooks, Linda. P. Dwoskin, and Roger L. Papke 2009. Inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel selective tris- and tetrakis-azaaromatic quaternary ammonium antagonists.Molecular Pharmacology76:652-66
- Hauser TA, Kucinski A, Jordan KG, Gatto GJ, Wersinger SR, Hesse RA, Stachowiak EK, Stachowiak MK, Papke RL, Lippiello PM, Bencherif M. 2009. An alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia.Biochemical Pharmacology78:803-12
- Reinhard David, Anna Ciuraszkiewicz, Xenia Simeone, Avi Orr-Urtreger, Roger L. Papke, Michael McIntosh, Sigismund Huck, and Petra Scholze 2010. Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes.European Journal of Neuroscience31:978-93
- Roger L. Papke Lynn Wecker and Jerry A. Stitzel. 2010. Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.Journal of Pharmacology and Experimental Therapeutics333:501-18
- Youyi Peng, Qiang Zhang, Gretchen Snyder, Hongwen Zhu, Wei Yao, John Tomesch, Roger L. Papke, James P. O’Callaghan, William J. Welsh, and Larry Wennogle. 2010. Discovery of Novel Alpha7 Nicotinic Receptor Antagonists.Bioorganic and Medicinal Chemistry Letters20:4825-30
- Roger L. Papke and Clare Stokes 2010. Working with OpusXpress: methods for high volume oocyte experiments.Methods51: 121-33
- Jingyi Wang, Nicole A. Horenstein, Clare Stokes, and Roger L. Papke. 2010. Tethered agonist analogs as site-specific probes for domains of human alpha7 nicotinic acetylcholine receptor that differentially regulate activation and desensitization.Molecular Pharmacology78:1012ñ1025
- Roger L. Papke, Caryn Trocme-Thibierge , Daniela Guendisch, Shehd Abdullah Abbas Al Rubaiy, and Stephen A. Bloom. 2011. Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists.Journal of Pharmacology and Experimental Therapeutics337:1-13
- Dustin K. Williams, Clare Stokes, Nicole A. Horenstein, and Roger L. Papke. 2011. The effective opening of nicotinic acetylcholine receptors with single agonist binding sites.Journal of General Physiology137:369-84
- Dustin K. Williams, Jingyi Wang, and Roger L. Papke. 2011. Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations..Biochemical Pharmacology82:915-30
- Dustin K. Williams, Jingyi Wang, and Roger L. Papke. 2011. Investigation of the molecular mechanism of the alpha7 nAChR positive allosteric modulator PNU-120596 provides evidence for two distinct desensitized states. Molecular Pharmacology 80:1013-32
- Roger L. Papke, Fumihito Ono, Clare Stokes, Jason Urban, and R. Thomas Boyd. 2012. The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study. Biochemical Pharmacology 84(3):352-65
- Jingyi Wang, Roger L. Papke, Clare Stokes, Nicole A. Horenstein. Potential state-selective hydrogen bond formation can modulate the activation and desensitization of the alpha7 nicotinic acetylcholine receptor. Molecular Pharmacology 81(2):21957-69
- Clare Stokes and Roger L. Papke. 2012. Use of an alpha3-beta4 nicotinic acetylcholine receptor subunit concatamer to characterize ganglionic receptor subtypes with specific subunit composition reveals species-specific pharmacologic properties. Neuropharmacology 63(4):538-46
- Teresa A. Murray, Daniel Bertrand, Roger L. Papke, Andrew A. George Rigo Pantoja, Rahul Srinivasan, Qiang Liu, Jie Wu, Paul Whiteaker, Henry A. Lester, Ronald J. Lukas. 2012. alpha7beta2nAChRs assemble and function, and are activated primarily via their alpha7 alpha7 interfaces. Molecular Pharmacology 81:175-88
- Dustin K. Williams, Can Peng, Matthew R. Kimbrell, Roger L. Papke. 2012. The intrinsically low open probability of alpha7 nAChR can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures. Molecular Pharmacology 82(4):746-59.
- Matthew D. Isaacson, Nicole A. Horenstein, Clare Stokes, William R. Kem, and Roger L. Papke. 2013. Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines. Biochemical Pharmacology 85(6):817-28
- Kinga Chojnacka, Roger L Papke, and Nicole A Horenstein. 2013. Synthesis and evaluation of a conditionally-silent agonist for the alpha7 nicotinic acetylcholine receptor. Bioorganic & Medicinal Chemistry Letters 23(14):4145-9.
- Can Peng, Matthew R. Kimbrell, Chengju Tian, Thomas F. Pack, Peter A. Crooks, E. Kim Fifer, and Roger L. Papke. 2013. Multiple modes of α7 nAChR non-competitive antagonism of control agonist-evoked and allosterically enhanced currents. Molecular Pharmacology 84(3):459-75.
- Can Peng, Clare Stokes, Yann S. Mineur, Marina R. Picciotto, Chengju Tian, Christoph Eibl, Isabelle Tomassoli, Daniela Guendisch and Roger L. Papke. 2013. Differential modulation of brain nicotinic acetylcholine receptor function by cytisine, varenicline and two novel bispidine compounds: Emergent properties of a hybrid molecule. Pharmacology and Experimental Therapeutics 347(2):424-37.
- Igari M, Alexander J.C., Bauzo R.M., Xiaoli Q., Papke R.L., Bruijnzeel A.W. 2013. Varenicline and cytisine diminish the dysphoria associated with nicotine withdrawal in rats. Neuropsycopharmacology in press
- Christoph Eibla, Isabelle Tomassoli, Clare Stokes, Roger L. Papke, Daniela Gundisch, 2013. The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor (nAChR) ligands: Part 1. The influence of different hydrogen bond acceptor systems on alkyl and (hetero)aryl substituents. Bioorganic and Medicinal Chemistry 21(23):7283-308.
- Christoph Eibl, Lenka Munoz, Isabelle Tomassoli, Clare Stokes, Roger L. Papke, Daniela Gundisch, 2013. The 3,7-Diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2. Carboxamide derivatives with different spacer motifs. Bioorganic and Medicinal Chemistry 21(23):7309-29.
- Ganesh A. Thakur, Abhijit R. Kulkarni, Jeffrey R. Deschamps, Roger L. Papke. 2013 Expeditious Synthesis, Enantiomeric Resolution and Enantiomer Functional Characterization of (4‐(4‐bromophenyl)‐3a, 4, 5, 9btetrahydro‐3H‐cyclopenta[c]-quinoline‐8‐sulfonamide (4BP‐TQS): an Allosteric agonist‐Positive Allosteric Modulator of alpha7 Nicotinic Acetylcholine Receptors. Journal of Medicinal Chemistry 56(21):8943–8947.
- Roger L. Papke, Clare Stokes, P. Muldoon, M. Imad Damaj. 2013 Similar activity of mecamylamine stereoisomers in vitro and in vivo. European Journal or Pharmacology 720(2013):264-75.
- Roger L. Papke, Nicole A. Horenstein, A. R. Kulkarni, Clare Stoke, L. W. Corrie, C. Y. Maeng, Ganesh A. Thakur. 2014. The activity of GAT107, an allosteric activator and positive modulator of alpha7 nAChR, is regulated by aromatic amino acids that span the subunit interface. Journal of Biochemistry.289(3):4515-31
- Roger L. Papke 2014. Merging old and new perspectives on nicotinic acetylcholine receptors. Biochemical Pharmacology89(1):1-11
- Roger L. Papke, Kinga Chojnacka, and Nicole A. Horenstein, 2014. The minimal pharmacophore for silent agonism of alpha7 nAChR.Journal of Pharmacology and Experimental Therapeutics350(3):665-680.
- Roger L Papke, Deniz Bagdas, Abhijit R Kulkarni, Timothy Gould, Shakir AlSharari, Ganesh A Thakur, and Imad M Damaj. 2015. The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with nonconducting conformations of the receptor.Neuropharmacology91(21):34-42.
- Marjolein A. van Maanen, Roger L. Papke, Frieda A. Koopman, Jessica Koepke, Lisette Bevaart, Roger Clark, Diana Lamppu, Daniel Elbaum, Gregory J. LaRosa, Paul P. Tak, and Margriet J. Vervoordeldonk. 2015 Two novel α7 nicotinic acetylcholine receptor ligands: in vitro properties and their efficacy in collagen-induced arthritis in mice. PLOS ONE 2014 January 24 10(1)
- Darlene H. Brunzell, J. Michael McIntosh and Roger L. Papke. Diverse strategies targeting alpha7 homomeric and alpha6beta2 heteromeric nicotinic acetylcholine receptors for smoking cessation. 2014.Annals of the New York Academy of Sciences132727-45
- Clare Stokes, Millet Treinin, and Roger L. Papke. Looking below the surface of nicotinic acetylcholine receptors. 2015.Trends in Pharmacological Sciences 36(8)514-23
- Melissa Little and Roger L. Papke. Betel, the orphan addiction. 2015. Journal of Addiction Research and Therapy 6(3): e130
- Roger L. Papke, Nicole A. Horenstein, and Clare Stokes. Nicotinic activity of arecoline, the psychoactive element of betel nuts, suggests a basis for habitual use and anti-inflammatory activity. 2015. PLoS One < b>10(10): e140907
- Nicole A. Horenstein, Roger L. Papke, Abhijit R. Kulkarni, Ganesh U. Chaturbhuj, Clare Stokes, Khan Manther and Ganesh A. Thakur. 2016. Critical molecular determinants of alpha7 nicotinic acetylcholine receptor allosteric activation: separation of direct allosteric activation and positive allosteric modulation. Journal of Biochemistry 291(10):5049-5067
- Deniz Bagdas, Jenny L. Wilkerson, Abhijit Kulkarni, Wisam Toma, Shakir AlSharari, Zulfiye Gul, Aron H. Lichtman, Roger L. Papke, Ganesh A. Thakur, and M. Imad Damaj. 2016. CThe alpha7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain. British Journal of Pharmacology 173(16):2506-20
