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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.


Distinct profiles of alpha7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes.

Grønlien JH, Håkerud M, Ween H, Thorin-Hagene K, Briggs CA, Gopalakrishnan M, Malysz J.

Mol Pharmacol. 2007 Sep;72(3):715-24. Epub 2007 Jun 12.


A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization.

Hurst RS, Hajós M, Raggenbass M, Wall TM, Higdon NR, Lawson JA, Rutherford-Root KL, Berkenpas MB, Hoffmann WE, Piotrowski DW, Groppi VE, Allaman G, Ogier R, Bertrand S, Bertrand D, Arneric SP.

J Neurosci. 2005 Apr 27;25(17):4396-405.


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.


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.


Mode of action of the positive modulator PNU-120596 on α7 nicotinic acetylcholine receptors.

Szabo AK, Pesti K, Mike A, Vizi ES.

Neuropharmacology. 2014 Jun;81:42-54. doi: 10.1016/j.neuropharm.2014.01.033. Epub 2014 Jan 31.


An Unaltered Orthosteric Site and a Network of Long-Range Allosteric Interactions for PNU-120596 in α7 Nicotinic Acetylcholine Receptors.

Marotta CB, Lester HA, Dougherty DA.

Chem Biol. 2015 Aug 20;22(8):1063-73. doi: 10.1016/j.chembiol.2015.06.018. Epub 2015 Jul 23.


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.


Evaluation of alpha7 nicotinic acetylcholine receptor agonists and positive allosteric modulators using the parallel oocyte electrophysiology test station.

Malysz J, Grønlien JH, Timmermann DB, Håkerud M, Thorin-Hagene K, Ween H, Trumbull JD, Xiong Y, Briggs CA, Ahring PK, Dyhring T, Gopalakrishnan M.

Assay Drug Dev Technol. 2009 Aug;7(4):374-90. doi: 10.1089/adt.2009.0194.


Competitive binding at a nicotinic receptor transmembrane site of two α7-selective positive allosteric modulators with differing effects on agonist-evoked desensitization.

Collins T, Young GT, Millar NS.

Neuropharmacology. 2011 Dec;61(8):1306-13. doi: 10.1016/j.neuropharm.2011.07.035. Epub 2011 Jul 30.


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.


In vivo pharmacological interactions between a type II positive allosteric modulator of α7 nicotinic ACh receptors and nicotinic agonists in a murine tonic pain model.

Freitas K, Negus SS, Carroll FI, Damaj MI.

Br J Pharmacol. 2013 Jun;169(3):567-79. doi: 10.1111/j.1476-5381.2012.02226.x.


Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.

Zhang Q, Du Y, Zhang J, Xu X, Xue F, Guo C, Huang Y, Lukas RJ, Chang Y.

PLoS One. 2015 Sep 4;10(9):e0137588. doi: 10.1371/journal.pone.0137588. eCollection 2015.


Development of Automated Patch Clamp Assay for Evaluation of α7 Nicotinic Acetylcholine Receptor Agonists in Automated QPatch-16.

Hao Y, Tang J, Wang K.

Assay Drug Dev Technol. 2015 Apr;13(3):174-84. doi: 10.1089/adt.2014.622. Epub 2015 Apr 16.


The chimeric gene CHRFAM7A, a partial duplication of the CHRNA7 gene, is a dominant negative regulator of α7*nAChR function.

Araud T, Graw S, Berger R, Lee M, Neveu E, Bertrand D, Leonard S.

Biochem Pharmacol. 2011 Oct 15;82(8):904-14. doi: 10.1016/j.bcp.2011.06.018. Epub 2011 Jun 28.

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