HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2021.113189 ◽

2021 ◽

Vol 214 ◽

pp. 113189

Author(s):

István Ledneczki ◽

Pál Tapolcsányi ◽

Eszter Gábor ◽

András Visegrády ◽

Márton Vass ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Scaffold Hopping ◽

Nicotinic Acetylcholine ◽

Advances in the Discovery of Novel Positive Allosteric Modulators of the α7 Nicotinic Acetylcholine Receptor

Recent Patents on CNS Drug Discovery ◽

10.2174/157488907780832751 ◽

2007 ◽

Vol 2 (2) ◽

Cited By ~ 27

Author(s):

Ramin Faghih ◽

Gregory A. Gfesser ◽

Murali Gopalakrishnan

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

3 α7 Nicotinic Acetylcholine Receptor Agonists and Positive Allosteric Modulators

Progress in Medicinal Chemistry - Progress in Medicinal Chemistry Volume 46 ◽

10.1016/s0079-6468(07)00003-3 ◽

2008 ◽

pp. 131-171 ◽

Cited By ~ 31

Author(s):

Andrew P. Lightfoot ◽

James N.C. Kew ◽

John Skidmore

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Receptor Agonists ◽

Characterization of the effects of novel positive allosteric modulators on the functionality of the α7 nicotinic acetylcholine receptor (nAChR)

The FASEB Journal ◽

10.1096/fasebj.2018.32.1_supplement.533.80 ◽

2018 ◽

Vol 32 (S1) ◽

Author(s):

Francis Reilly‐Andujar ◽

José A. Lasalde ◽

José O. Colón

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Positive allosteric modulators of the α7 nicotinic acetylcholine receptor potentiate glutamate release in the prefrontal cortex of freely-moving rats

Neuropharmacology ◽

10.1016/j.neuropharm.2016.08.033 ◽

2016 ◽

Vol 111 ◽

pp. 78-91 ◽

Cited By ~ 3

Author(s):

D.M. Bortz ◽

B.A. Upton ◽

J.D. Mikkelsen ◽

J.P. Bruno

Keyword(s):

Prefrontal Cortex ◽

Acetylcholine Receptor ◽

Glutamate Release ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Freely Moving Rats ◽

Freely Moving ◽

Repeated administration of α7 nicotinic acetylcholine receptor (nAChR) agonists, but not positive allosteric modulators, increases α7 nAChR levels in the brain

Journal of Neurochemistry ◽

10.1111/j.1471-4159.2010.06845.x ◽

2010 ◽

pp. no-no ◽

Cited By ~ 1

Author(s):

Ditte Z. Christensen ◽

Jens D. Mikkelsen ◽

Henrik H. Hansen ◽

Morten S. Thomsen

Keyword(s):

Acetylcholine Receptor ◽

Repeated Administration ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Α7 Nachr ◽

Positive Allosteric Modulators ◽

The Brain

Novel Positive Allosteric Modulators of the Human α7 Nicotinic Acetylcholine Receptor

Biochemistry ◽

10.1021/bi102001m ◽

2011 ◽

Vol 50 (23) ◽

pp. 5263-5278 ◽

Cited By ~ 37

Author(s):

Hugo R. Arias ◽

Ruo-Xu Gu ◽

Dominik Feuerbach ◽

Bao-Bao Guo ◽

Yong Ye ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Antinociceptive effects of α7 nicotinic acetylcholine receptor positive allosteric modulators type I and II in models of acute and chronic pain in mice

The FASEB Journal ◽

10.1096/fasebj.27.1_supplement.886.14 ◽

2013 ◽

Vol 27 (S1) ◽

Author(s):

Kelen Freitas ◽

S Stevens Negus ◽

F Ivy Carroll ◽

M Imad Damaj

Keyword(s):

Chronic Pain ◽

Acetylcholine Receptor ◽

Type I ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Antinociceptive Effects ◽

Evaluation of α7 Nicotinic Acetylcholine Receptor Agonists and Positive Allosteric Modulators Using the Parallel Oocyte Electrophysiology Test Station

Assay and Drug Development Technologies ◽

10.1089/adt.2009.0194 ◽

2009 ◽

Vol 7 (4) ◽

pp. 374-390 ◽

Cited By ~ 21

Author(s):

John Malysz ◽

Jens H. Grønlien ◽

Daniel B. Timmermann ◽

Monika Håkerud ◽

Kirsten Thorin-Hagene ◽

...

Keyword(s):

Acetylcholine Receptor ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽

Receptor Agonists ◽

Positive Allosteric Modulators ◽

Electrophysiology Test

Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model

Molecular Pharmacology ◽

10.1124/mol.117.110551 ◽

2017 ◽

Vol 93 (2) ◽

pp. 128-140 ◽

Cited By ~ 23

Author(s):

Joseph Newcombe ◽

Anna Chatzidaki ◽

Tom D. Sheppard ◽

Maya Topf ◽

Neil S. Millar

Keyword(s):

Acetylcholine Receptor ◽

Structural Model ◽

Allosteric Modulators ◽

Nicotinic Acetylcholine ◽