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NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity.

Papke RL, Peng C, Kumar A, Stokes C.

Neurosci Lett. 2018 Jun 11;677:6-13. doi: 10.1016/j.neulet.2018.04.025. Epub 2018 Apr 19.


Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal.

Jackson A, Papke RL, Damaj MI.

Psychopharmacology (Berl). 2018 Jul;235(7):1897-1905. doi: 10.1007/s00213-018-4879-7. Epub 2018 Mar 16.


Cracking the Betel Nut: Cholinergic Activity of Areca Alkaloids and Related Compounds.

Horenstein NA, Quadri M, Stokes C, Shoaib M, Papke RL.

Nicotine Tob Res. 2017 Oct 3. doi: 10.1093/ntr/ntx187. [Epub ahead of print]


Anti-inflammatory Silent Agonists.

Horenstein NA, Papke RL.

ACS Med Chem Lett. 2017 Sep 26;8(10):989-991. doi: 10.1021/acsmedchemlett.7b00368. eCollection 2017 Oct 12.


Rabies virus modifies host behaviour through a snake-toxin like region of its glycoprotein that inhibits neurotransmitter receptors in the CNS.

Hueffer K, Khatri S, Rideout S, Harris MB, Papke RL, Stokes C, Schulte MK.

Sci Rep. 2017 Oct 9;7(1):12818. doi: 10.1038/s41598-017-12726-4.


Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.

Quadri M, Stokes C, Gulsevin A, Felts ACJ, Abboud KA, Papke RL, Horenstein NA.

J Med Chem. 2017 Sep 28;60(18):7928-7934. doi: 10.1021/acs.jmedchem.7b00875. Epub 2017 Sep 14.


Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.

Jin Y, Huang X, Papke RL, Jutkiewicz EM, Showalter HD, Zhan CG.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4350-4353. doi: 10.1016/j.bmcl.2017.08.025. Epub 2017 Aug 14.


New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs.

Bagdas D, Gurun MS, Flood P, Papke RL, Damaj MI.

Curr Neuropharmacol. 2018;16(4):415-425. doi: 10.2174/1570159X15666170818102108.


The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.

Donvito G, Bagdas D, Toma W, Rahimpour E, Jackson A, Meade JA, AlSharari S, Kulkarni AR, Ivy Carroll F, Lichtman AH, Papke RL, Thakur GA, Imad Damaj M.

Exp Neurol. 2017 Sep;295:194-201. doi: 10.1016/j.expneurol.2017.06.014. Epub 2017 Jun 9.


Identification of α7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine-Δ2 -Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation.

Quadri M, Matera C, Silnović A, Pismataro MC, Horenstein NA, Stokes C, Papke RL, Dallanoce C.

ChemMedChem. 2017 Aug 22;12(16):1335-1348. doi: 10.1002/cmdc.201700162. Epub 2017 Jun 12.


Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.

Papke RL, Stokes C, Damaj MI, Thakur GA, Manther K, Treinin M, Bagdas D, Kulkarni AR, Horenstein NA.

Br J Pharmacol. 2018 Jun;175(11):1838-1854. doi: 10.1111/bph.13851. Epub 2017 Jun 8.


Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (-)-[(18)F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain.

Hillmer AT, Esterlis I, Gallezot JD, Bois F, Zheng MQ, Nabulsi N, Lin SF, Papke RL, Huang Y, Sabri O, Carson RE, Cosgrove KP.

Neuroimage. 2016 Nov 1;141:71-80. doi: 10.1016/j.neuroimage.2016.07.026. Epub 2016 Jul 15.


The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.

Bagdas D, Wilkerson JL, Kulkarni A, Toma W, AlSharari S, Gul Z, Lichtman AH, Papke RL, Thakur GA, Damaj MI.

Br J Pharmacol. 2016 Aug;173(16):2506-20. doi: 10.1111/bph.13528. Epub 2016 Jul 18.


Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.

Horenstein NA, Papke RL, Kulkarni AR, Chaturbhuj GU, Stokes C, Manther K, Thakur GA.

J Biol Chem. 2016 Mar 4;291(10):5049-67. doi: 10.1074/jbc.M115.692392. Epub 2016 Jan 7.


Dissection of N,N-diethyl-N'-phenylpiperazines as α7 nicotinic receptor silent agonists.

Quadri M, Papke RL, Horenstein NA.

Bioorg Med Chem. 2016 Jan 15;24(2):286-93. doi: 10.1016/j.bmc.2015.12.017. Epub 2015 Dec 9.


Nicotinic Activity of Arecoline, the Psychoactive Element of "Betel Nuts", Suggests a Basis for Habitual Use and Anti-Inflammatory Activity.

Papke RL, Horenstein NA, Stokes C.

PLoS One. 2015 Oct 21;10(10):e0140907. doi: 10.1371/journal.pone.0140907. eCollection 2015.


Looking below the surface of nicotinic acetylcholine receptors.

Stokes C, Treinin M, Papke RL.

Trends Pharmacol Sci. 2015 Aug;36(8):514-23. doi: 10.1016/ Epub 2015 Jun 8. Review.


Two novel α7 nicotinic acetylcholine receptor ligands: in vitro properties and their efficacy in collagen-induced arthritis in mice.

van Maanen MA, Papke RL, Koopman FA, Koepke J, Bevaart L, Clark R, Lamppu D, Elbaum D, LaRosa GJ, Tak PP, Vervoordeldonk MJ.

PLoS One. 2015 Jan 24;10(1):e0116227. doi: 10.1371/journal.pone.0116227. eCollection 2015.


The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.

Papke RL, Bagdas D, Kulkarni AR, Gould T, AlSharari SD, Thakur GA, Damaj MI.

Neuropharmacology. 2015 Apr;91:34-42. doi: 10.1016/j.neuropharm.2014.12.002. Epub 2014 Dec 11.


The α7 nicotinic receptor agonist ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions.

Bordia T, McGregor M, Papke RL, Decker MW, McIntosh JM, Quik M.

Exp Neurol. 2015 Jan;263:277-84. doi: 10.1016/j.expneurol.2014.09.015. Epub 2014 Sep 28.


The minimal pharmacophore for silent agonism of the α7 nicotinic acetylcholine receptor.

Papke RL, Chojnacka K, Horenstein NA.

J Pharmacol Exp Ther. 2014 Sep;350(3):665-80. doi: 10.1124/jpet.114.215236. Epub 2014 Jul 2. Erratum in: J Pharmacol Exp Ther. 2015 Sep;354(3):483.


The cytisine derivatives, CC4 and CC26, reduce nicotine-induced conditioned place preference in zebrafish by acting on heteromeric neuronal nicotinic acetylcholine receptors.

Ponzoni L, Braida D, Pucci L, Andrea D, Fasoli F, Manfredi I, Papke RL, Stokes C, Cannazza G, Clementi F, Gotti C, Sala M.

Psychopharmacology (Berl). 2014 Dec;231(24):4681-93. doi: 10.1007/s00213-014-3619-x. Epub 2014 May 27.


Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation.

Brunzell DH, McIntosh JM, Papke RL.

Ann N Y Acad Sci. 2014 Oct;1327:27-45. doi: 10.1111/nyas.12421. Epub 2014 Apr 14. Review.


Merging old and new perspectives on nicotinic acetylcholine receptors.

Papke RL.

Biochem Pharmacol. 2014 May 1;89(1):1-11. doi: 10.1016/j.bcp.2014.01.029. Epub 2014 Jan 31. Review.


Rare human nicotinic acetylcholine receptor α4 subunit (CHRNA4) variants affect expression and function of high-affinity nicotinic acetylcholine receptors.

McClure-Begley TD, Papke RL, Stone KL, Stokes C, Levy AD, Gelernter J, Xie P, Lindstrom J, Picciotto MR.

J Pharmacol Exp Ther. 2014 Mar;348(3):410-20. doi: 10.1124/jpet.113.209767. Epub 2014 Jan 2.


The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.

Papke RL, Horenstein NA, Kulkarni AR, Stokes C, Corrie LW, Maeng CY, Thakur GA.

J Biol Chem. 2014 Feb 14;289(7):4515-31. doi: 10.1074/jbc.M113.524603. Epub 2013 Dec 20.


Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration.

Eskildsen J, Redrobe JP, Sams AG, Dekermendjian K, Laursen M, Boll JB, Papke RL, Bundgaard C, Frederiksen K, Bastlund JF.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):288-93. doi: 10.1016/j.bmcl.2013.11.022. Epub 2013 Nov 20.


Similar activity of mecamylamine stereoisomers in vitro and in vivo.

Papke RL, Stokes C, Muldoon P, Imad Damaj M.

Eur J Pharmacol. 2013 Nov 15;720(1-3):264-75. doi: 10.1016/j.ejphar.2013.10.018. Epub 2013 Oct 23.


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.

Eibl C, Tomassoli I, Munoz L, Stokes C, Papke RL, Gündisch D.

Bioorg Med Chem. 2013 Dec 1;21(23):7283-308. doi: 10.1016/j.bmc.2013.09.059. Epub 2013 Oct 5.


The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs.

Eibl C, Munoz L, Tomassoli I, Stokes C, Papke RL, Gündisch D.

Bioorg Med Chem. 2013 Dec 1;21(23):7309-29. doi: 10.1016/j.bmc.2013.09.060. Epub 2013 Oct 5.


Varenicline and cytisine diminish the dysphoric-like state associated with spontaneous nicotine withdrawal in rats.

Igari M, Alexander JC, Ji Y, Qi X, Papke RL, Bruijnzeel AW.

Neuropsychopharmacology. 2014 Jan;39(2):455-65. doi: 10.1038/npp.2013.216. Epub 2013 Aug 21.


Differential modulation of brain nicotinic acetylcholine receptor function by cytisine, varenicline, and two novel bispidine compounds: emergent properties of a hybrid molecule.

Peng C, Stokes C, Mineur YS, Picciotto MR, Tian C, Eibl C, Tomassoli I, Guendisch D, Papke RL.

J Pharmacol Exp Ther. 2013 Nov;347(2):424-37. doi: 10.1124/jpet.113.206904. Epub 2013 Aug 19.


Multiple modes of α7 nAChR noncompetitive antagonism of control agonist-evoked and allosterically enhanced currents.

Peng C, Kimbrell MR, Tian C, Pack TF, Crooks PA, Fifer EK, Papke RL.

Mol Pharmacol. 2013 Sep;84(3):459-75. doi: 10.1124/mol.113.086462. Epub 2013 Jul 9.


Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor.

Chojnacka K, Papke RL, Horenstein NA.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4145-9. doi: 10.1016/j.bmcl.2013.05.039. Epub 2013 May 23.


Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines.

Isaacson MD, Horenstein NA, Stokes C, Kem WR, Papke RL.

Biochem Pharmacol. 2013 Mar 15;85(6):817-28. doi: 10.1016/j.bcp.2013.01.010. Epub 2013 Jan 23.


The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study.

Papke RL, Ono F, Stokes C, Urban JM, Boyd RT.

Biochem Pharmacol. 2012 Aug 1;84(3):352-65. doi: 10.1016/j.bcp.2012.04.022. Epub 2012 May 10.


Potential state-selective hydrogen bond formation can modulate activation and desensitization of the α7 nicotinic acetylcholine receptor.

Wang J, Papke RL, Stokes C, Horenstein NA.

J Biol Chem. 2012 Jun 22;287(26):21957-69. doi: 10.1074/jbc.M112.339796. Epub 2012 May 3.


α7β2 nicotinic acetylcholine receptors assemble, function, and are activated primarily via their α7-α7 interfaces.

Murray TA, Bertrand D, Papke RL, George AA, Pantoja R, Srinivasan R, Liu Q, Wu J, Whiteaker P, Lester HA, Lukas RJ.

Mol Pharmacol. 2012 Feb;81(2):175-88. doi: 10.1124/mol.111.074088. Epub 2011 Oct 28. Erratum in: Mol Pharmacol. 2016 Sep;90(3):410.


Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.

Williams DK, Wang J, Papke RL.

Biochem Pharmacol. 2011 Oct 15;82(8):915-30. doi: 10.1016/j.bcp.2011.05.001. Epub 2011 May 14. Review.


The effective opening of nicotinic acetylcholine receptors with single agonist binding sites.

Williams DK, Stokes C, Horenstein NA, Papke RL.

J Gen Physiol. 2011 Apr;137(4):369-84. doi: 10.1085/jgp.201010587.


Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists.

Papke RL, Trocmé-Thibierge C, Guendisch D, Al Rubaiy SA, Bloom SA.

J Pharmacol Exp Ther. 2011 May;337(2):367-79. doi: 10.1124/jpet.110.177485. Epub 2011 Feb 1.


Tethered agonist analogs as site-specific probes for domains of the human α7 nicotinic acetylcholine receptor that differentially regulate activation and desensitization.

Wang J, Horenstein NA, Stokes C, Papke RL.

Mol Pharmacol. 2010 Dec;78(6):1012-25. doi: 10.1124/mol.110.066662. Epub 2010 Sep 7.


Cysteine accessibility analysis of the human alpha7 nicotinic acetylcholine receptor ligand-binding domain identifies L119 as a gatekeeper.

Papke RL, Stokes C, Williams DK, Wang J, Horenstein NA.

Neuropharmacology. 2011 Jan;60(1):159-71. doi: 10.1016/j.neuropharm.2010.07.014. Epub 2010 Jul 27.


alpha4beta2 Nicotinic acetylcholine receptors, willing if able.

Papke RL.

Br J Pharmacol. 2010 Aug;160(8):1903-5. doi: 10.1111/j.1476-5381.2010.00868.x.


Discovery of novel alpha7 nicotinic receptor antagonists.

Peng Y, Zhang Q, Snyder GL, Zhu H, Yao W, Tomesch J, Papke RL, O'Callaghan JP, Welsh WJ, Wennogle LP.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4825-30. doi: 10.1016/j.bmcl.2010.06.103. Epub 2010 Jun 25.

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