Roger Papke


Affiliation: University of Florida
Country: USA


  1. request reprint
    Papke R, McCormack T, Jack B, Wang D, Bugaj Gaweda B, Schiff H, et al. Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytes. Eur J Pharmacol. 2005;524:11-8 pubmed
    ..They also point to the potential importance of a newly identified sequence element for modeling the specific amino acids involved with receptor activation. ..
  2. Quadri M, Garai S, Thakur G, Stokes C, Gulsevin A, Horenstein N, et al. Macroscopic and microscopic activation of α7 nicotinic acetylcholine receptors by the structurally unrelated ago-PAMs B-973B and GAT107. Mol Pharmacol. 2018;: pubmed publisher
    ..Modeling and docking studies suggest that the molecular basis for these effects depends on specific interactions in both the extracellular and transmembrane domains of the receptor. ..
  3. Quadri M, Bagdas D, Toma W, Stokes C, Horenstein N, Damaj M, et al. The antinociceptive and anti-inflammatory properties of the ?7 nAChR weak partial agonist p-CF3N,N-diethyl-N'-phenylpiperazine. J Pharmacol Exp Ther. 2018;: pubmed publisher
    ..The compound was effective in a mouse chronic neuropathic model, and its effects were mediated by ?7, thus proving its potential therapeutic use in inflammatory diseases. ..
  4. Papke R, Smith Maxwell C. High throughput electrophysiology with Xenopus oocytes. Comb Chem High Throughput Screen. 2009;12:38-50 pubmed
    ..We show some types of data that have been gathered by this system and review realized and potential applications. ..
  5. Papke R, Kem W, Soti F, López Hernández G, Horenstein N. Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine. J Pharmacol Exp Ther. 2009;329:791-807 pubmed publisher
  6. Papke R, Trocme Thibierge C, Guendisch D, Al Rubaiy S, Bloom S. Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists. J Pharmacol Exp Ther. 2011;337:367-79 pubmed publisher
    ..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. ..
  7. Stokes C, Treinin M, Papke R. Looking below the surface of nicotinic acetylcholine receptors. Trends Pharmacol Sci. 2015;36:514-23 pubmed publisher
    ..There are potential phosphorylation and protein-binding sites in the α7 intracellular domain, which are conserved and may be the basis for α7-mediated signal transduction. ..
  8. Papke R, Peng C, Kumar A, Stokes C. NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity. Neurosci Lett. 2018;677:6-13 pubmed publisher
    ..The results support the hypothesis that NS6740 switches the mode of α7 signaling in a channel-independent manner that can reduce synaptic function. ..
  9. Papke R, Dwoskin L, Crooks P, Zheng G, Zhang Z, McIntosh J, et al. Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras. Neuropharmacology. 2008;54:1189-200 pubmed publisher
    ..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. ..

More Information


  1. request reprint
    Papke R, Dwoskin L, Crooks P. The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discovery. J Neurochem. 2007;101:160-7 pubmed
    ..Thus, understanding the actions of nornicotine in the brain may have significance for both emerging therapeutics and the management of nicotine dependence. ..
  2. Papke R, Wecker L, Stitzel J. Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes. J Pharmacol Exp Ther. 2010;333:501-18 pubmed publisher
    ..Hexamethonium was a relatively nonselective antagonist with mixed competitive and noncompetitive activity...
  3. Papke R, Ono F, Stokes C, Urban J, Boyd R. The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study. Biochem Pharmacol. 2012;84:352-65 pubmed publisher
    ..Our data therefore indicate that while some pharmacological tools used in zebrafish may function as expected, others will not. ..