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Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling.

Papke RL, Lindstrom JM.

Neuropharmacology. 2020 May 15;168:108021. doi: 10.1016/j.neuropharm.2020.108021. Epub 2020 Feb 28. Review.


The α7 nicotinic acetylcholine receptor positive allosteric modulator prevents lipopolysaccharide-induced allodynia, hyperalgesia and TNF-α in the hippocampus in mice.

Abbas M, Alzarea S, Papke RL, Rahman S.

Pharmacol Rep. 2019 Nov;71(6):1168-1176. doi: 10.1016/j.pharep.2019.07.001. Epub 2019 Jul 3.


In silico modeling of the α7 nicotinic acetylcholine receptor: new pharmacological challenges associated with multiple modes of signaling.

Gulsevin A, Papke RL, Horenstein N.

Mini Rev Med Chem. 2020 Jan 29. doi: 10.2174/1389557520666200130105256. [Epub ahead of print]


A silent agonist of α7 nicotinic acetylcholine receptors modulates inflammation ex vivo and attenuates EAE.

Godin JR, Roy P, Quadri M, Bagdas D, Toma W, Narendrula-Kotha R, Kishta OA, Damaj MI, Horenstein NA, Papke RL, Simard AR.

Brain Behav Immun. 2019 Dec 23. pii: S0889-1591(19)31074-8. doi: 10.1016/j.bbi.2019.12.014. [Epub ahead of print]


Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs.

Camacho-Hernandez GA, Stokes C, Duggan BM, Kaczanowska K, Brandao-Araiza S, Doan L, Papke RL, Taylor P.

J Med Chem. 2019 Nov 27;62(22):10376-10390. doi: 10.1021/acs.jmedchem.9b01467. Epub 2019 Nov 19.


The α7 nicotinic acetylcholine receptor positive allosteric modulator prevents lipopolysaccharide-induced allodynia, hyperalgesia and TNF-α in the hippocampus in mice.

Abbas M, Alzarea S, Papke RL, Rahman S.

Pharmacol Rep. 2019 Dec;71(6):1168-1176. doi: 10.1016/j.pharep.2019.07.001. Epub 2019 Jul 3.


Impact of modulation of the α7 nicotinic acetylcholine receptor on nicotine reward in the mouse conditioned place preference test.

Jackson A, Alkhlaif Y, Papke RL, Brunzell DH, Damaj MI.

Psychopharmacology (Berl). 2019 Dec;236(12):3593-3599. doi: 10.1007/s00213-019-05331-y. Epub 2019 Jul 13.


The α7 nicotinic receptor silent agonist R-47 prevents and reverses paclitaxel-induced peripheral neuropathy in mice without tolerance or altering nicotine reward and withdrawal.

Toma W, Kyte SL, Bagdas D, Jackson A, Meade JA, Rahman F, Chen ZJ, Del Fabbro E, Cantwell L, Kulkarni A, Thakur GA, Papke RL, Bigbee JW, Gewirtz DA, Damaj MI.

Exp Neurol. 2019 Oct;320:113010. doi: 10.1016/j.expneurol.2019.113010. Epub 2019 Jul 9.


Betel Nut (areca) and Smokeless Tobacco Use in Myanmar.

Papke RL, Bhattacharyya I, Hatsukami DK, Moe I, Glatman S.

Subst Use Misuse. 2019 Jun 20:1-10. doi: 10.1080/10826084.2019.1624774. [Epub ahead of print] Erratum in: Subst Use Misuse. 2019;54(14):2425.


Heteromeric Neuronal Nicotinic Acetylcholine Receptors with Mutant β Subunits Acquire Sensitivity to α7-Selective Positive Allosteric Modulators.

Stokes C, Garai S, Kulkarni AR, Cantwell LN, Noviello CM, Hibbs RE, Horenstein NA, Abboud KA, Thakur GA, Papke RL.

J Pharmacol Exp Ther. 2019 Aug;370(2):252-268. doi: 10.1124/jpet.119.259499. Epub 2019 Jun 7.


Allosteric Agonism of α7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site.

Gulsevin A, Papke RL, Stokes C, Garai S, Thakur GA, Quadri M, Horenstein NA.

Mol Pharmacol. 2019 Jun;95(6):606-614. doi: 10.1124/mol.119.115758. Epub 2019 Apr 3.


B-973, a Novel α7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and in Vivo Evaluation.

Garai S, Raja KS, Papke RL, Deschamps JR, Damaj MI, Thakur GA.

ACS Med Chem Lett. 2018 Oct 11;9(11):1144-1148. doi: 10.1021/acsmedchemlett.8b00407. eCollection 2018 Nov 8.


Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107.

Quadri M, Garai S, Thakur GA, Stokes C, Gulsevin A, Horenstein NA, Papke RL.

Mol Pharmacol. 2019 Jan;95(1):43-61. doi: 10.1124/mol.118.113340. Epub 2018 Oct 22.


Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.

Quadri M, Silnović A, Matera C, Horenstein NA, Stokes C, De Amici M, Papke RL, Dallanoce C.

Eur J Med Chem. 2018 Dec 5;160:207-228. doi: 10.1016/j.ejmech.2018.10.015. Epub 2018 Oct 11.


The Antinociceptive and Anti-Inflammatory Properties of the α7 nAChR Weak Partial Agonist p-CF3 N,N-diethyl-N'-phenylpiperazine.

Quadri M, Bagdas D, Toma W, Stokes C, Horenstein NA, Damaj MI, Papke RL.

J Pharmacol Exp Ther. 2018 Nov;367(2):203-214. doi: 10.1124/jpet.118.249904. Epub 2018 Aug 15.


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. 2019 May 21;21(6):805-812. doi: 10.1093/ntr/ntx187.


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. Review.


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.


Role of the α7 Nicotinic Acetylcholine Receptor and RIC-3 in the Cholinergic Anti-inflammatory Pathway.

Treinin M, Papke RL, Nizri E, Ben-David Y, Mizrachi T, Brenner T.

Cent Nerv Syst Agents Med Chem. 2017;17(2):90-99. doi: 10.2174/1871524916666160829114533. Review.


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.

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