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Items: 36


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.


Characterization of the PLP-dependent transaminase initiating azasugar biosynthesis.

Arciola JM, Horenstein NA.

Biochem J. 2018 Jul 17;475(13):2241-2256. doi: 10.1042/BCJ20180340.


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.


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.


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.


Experimental and Metabolic Modeling Evidence for a Folate-Cleaving Side-Activity of Ketopantoate Hydroxymethyltransferase (PanB).

Thiaville JJ, Frelin O, García-Salinas C, Harrison K, Hasnain G, Horenstein NA, Díaz de la Garza RI, Henry CS, Hanson AD, de Crécy-Lagard V.

Front Microbiol. 2016 Mar 31;7:431. doi: 10.3389/fmicb.2016.00431. eCollection 2016.


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.


Infrared multiple photon dissociation spectrum of protonated bis(2-methoxyethyl) ether obtained with a tunable CO2 laser.

Ehsan MU, Bozai Y, Pearson WL 3rd, Horenstein NA, Eyler JR.

Phys Chem Chem Phys. 2015 Oct 21;17(39):25877-81. doi: 10.1039/c5cp01752a.


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 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.


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.


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.


Free energy study of the catalytic mechanism of Trypanosoma cruzi trans-sialidase. From the Michaelis complex to the covalent intermediate.

Pierdominici-Sottile G, Horenstein NA, Roitberg AE.

Biochemistry. 2011 Nov 22;50(46):10150-8. doi: 10.1021/bi2009618. Epub 2011 Oct 27.


Identification of a gene cluster that initiates azasugar biosynthesis in Bacillus amyloliquefaciens.

Clark LF, Johnson JV, Horenstein NA.

Chembiochem. 2011 Sep 19;12(14):2147-50. doi: 10.1002/cbic.201100347. Epub 2011 Jul 22. No abstract available.


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.


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.


Detecting extracellular carbonic anhydrase activity using membrane inlet mass spectrometry.

Delacruz J, Mikulski R, Tu C, Li Y, Wang H, Shiverick KT, Frost SC, Horenstein NA, Silverman DN.

Anal Biochem. 2010 Aug;403(1-2):74-8. doi: 10.1016/j.ab.2010.04.019. Epub 2010 Apr 22.


Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site.

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

J Pharmacol Exp Ther. 2009 Jul;330(1):40-53. doi: 10.1124/jpet.109.151225. Epub 2009 Apr 1.


Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine.

Papke RL, Kem WR, Soti F, López-Hernández GY, Horenstein NA.

J Pharmacol Exp Ther. 2009 May;329(2):791-807. doi: 10.1124/jpet.108.150151. Epub 2009 Feb 17.


Synthesis of H-bonding probes of alpha7 nAChR agonist selectivity.

Wang J, Papke RL, Horenstein NA.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):474-6. doi: 10.1016/j.bmcl.2008.11.044. Epub 2008 Nov 18.


Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors.

Horenstein NA, Leonik FM, Papke RL.

Mol Pharmacol. 2008 Dec;74(6):1496-511. doi: 10.1124/mol.108.048892. Epub 2008 Sep 2.


Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.

Leonik FM, Papke RL, Horenstein NA.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1520-2. Epub 2007 Jan 12.


Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors.

Horenstein NA, McCormack TJ, Stokes C, Ren K, Papke RL.

J Biol Chem. 2007 Feb 23;282(8):5899-909. Epub 2006 Dec 21.


Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist.

Papke RL, Schiff HC, Jack BA, Horenstein NA.

Neurosci Lett. 2005 Apr 22;378(3):140-4. Epub 2005 Jan 5.


The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker 2,2,6,6-tetramethylpiperidin-4-yl heptanoate.

Papke RL, Buhr JD, Francis MM, Choi KI, Thinschmidt JS, Horenstein NA.

Mol Pharmacol. 2005 Jun;67(6):1977-90. Epub 2005 Mar 10.


The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors.

Stokes C, Papke JK, Horenstein NA, Kem WR, McCormack TJ, Papke RL.

Mol Pharmacol. 2004 Jul;66(1):14-24.


Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy.

Papke RL, Meyer EM, Lavieri S, Bollampally SR, Papke TA, Horenstein NA, Itoh Y, Porter Papke JK.

Neuropharmacology. 2004 Jun;46(7):1023-38.


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