Literature DB >> 20638843

Discovery of novel alpha7 nicotinic receptor antagonists.

Youyi Peng1, Qiang Zhang, Gretchen L Snyder, Hongwen Zhu, Wei Yao, John Tomesch, Roger L Papke, James P O'Callaghan, William J Welsh, Lawrence P Wennogle.   

Abstract

Two distinct families of small molecules were discovered as novel alpha7 nicotinic acetylcholine receptor (nAChR) antagonists by pharmacophore-based virtual screening. These novel antagonists exhibited selectivity for the neuronal alpha7 subtype over other nAChRs and good brain penetration. Neuroprotection was demonstrated by representative compounds 7i and 8 in a mouse seizure-like behavior model induced by the nerve agent diisopropylfluorophosphate (DFP). These novel nAChR antagonists have potential use as antidote for organophosphorus nerve agent intoxication. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20638843      PMCID： PMC3000800          DOI： 10.1016/j.bmcl.2010.06.103

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  31 in total

Review 1.  International Union of Pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits.

Authors:  R J Lukas; J P Changeux; N Le Novère; E X Albuquerque; D J Balfour; D K Berg; D Bertrand; V A Chiappinelli; P B Clarke; A C Collins; J A Dani; S R Grady; K J Kellar; J M Lindstrom; M J Marks; M Quik; P W Taylor; S Wonnacott
Journal:  Pharmacol Rev       Date:  1999-06       Impact factor: 25.468

2.  Proof-of-concept trial of an alpha7 nicotinic agonist in schizophrenia.

Authors:  Ann Olincy; Josette G Harris; Lynn L Johnson; Vicki Pender; Susan Kongs; Diana Allensworth; Jamey Ellis; Gary O Zerbe; Sherry Leonard; Karen E Stevens; James O Stevens; Laura Martin; Lawrence E Adler; Ferenc Soti; William R Kem; Robert Freedman
Journal:  Arch Gen Psychiatry       Date:  2006-06

Review 3.  Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.

Authors:  Anders A Jensen; Bente Frølund; Tommy Liljefors; Povl Krogsgaard-Larsen
Journal:  J Med Chem       Date:  2005-07-28       Impact factor: 7.446

Review 4.  Selective alpha7 nicotinic acetylcholine receptor ligands.

Authors:  Anatoly Mazurov; Terry Hauser; Craig H Miller
Journal:  Curr Med Chem       Date:  2006       Impact factor: 4.530

Review 5.  Strategies for compound selection.

Authors:  Marius M Olah; Cristian G Bologa; Tudor I Oprea
Journal:  Curr Drug Discov Technol       Date:  2004-10

6.  Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.

Authors:  Alice L Bodnar; Luz A Cortes-Burgos; Karen K Cook; Dac M Dinh; Vincent E Groppi; Mihaly Hajos; Nicole R Higdon; William E Hoffmann; Raymond S Hurst; Jason K Myers; Bruce N Rogers; Theron M Wall; Mark L Wolfe; Erik Wong
Journal:  J Med Chem       Date:  2005-02-24       Impact factor: 7.446

7.  Conformational sampling of druglike molecules with MOE and catalyst: implications for pharmacophore modeling and virtual screening.

Authors:  I-Jen Chen; Nicolas Foloppe
Journal:  J Chem Inf Model       Date:  2008-09-03       Impact factor: 4.956

8.  The novel alpha7 nicotinic acetylcholine receptor agonist N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-7-[2-(methoxy)phenyl]-1-benzofuran-2-carboxamide improves working and recognition memory in rodents.

Authors:  Frank G Boess; Jean De Vry; Christina Erb; Timo Flessner; Martin Hendrix; Joachim Luithle; Christoph Methfessel; Bernd Riedl; Katrin Schnizler; Franz-Josef van der Staay; Marja van Kampen; Welf Burkhard Wiese; Gerhard Koenig
Journal:  J Pharmacol Exp Ther       Date:  2007-02-16       Impact factor: 4.030

Review 9.  Neuronal nicotinic receptors: a perspective on two decades of drug discovery research.

Authors:  Stephen P Arneric; Mark Holladay; Michael Williams
Journal:  Biochem Pharmacol       Date:  2007-06-26       Impact factor: 5.858

10.  Selective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonists.

Authors:  Gretchen Y López-Hernández; Jeffrey S Thinschmidt; Guangrong Zheng; Zhenfa Zhang; Peter A Crooks; Linda P Dwoskin; Roger L Papke
Journal:  Mol Pharmacol       Date:  2009-06-25       Impact factor: 4.436
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  4 in total

1.  Stable expression and functional characterization of a human nicotinic acetylcholine receptor with α6β2 properties: discovery of selective antagonists.

Authors:  Anna Maria Capelli; Laura Castelletti; Yu Hua Chen; Harjeet Van der Keyl; Luca Pucci; Beatrice Oliosi; Cristian Salvagno; Barbara Bertani; Cecilia Gotti; Andrew Powell; Manolo Mugnaini
Journal:  Br J Pharmacol       Date:  2011-05       Impact factor: 8.739

Review 2.  Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors.

Authors:  Roger L Papke; Nicole A Horenstein
Journal:  Pharmacol Rev       Date:  2021-07       Impact factor: 18.923

3.  Methylpiperidinium Iodides as Novel Antagonists for α7 Nicotinic Acetylcholine Receptors.

Authors:  Jhon J López; Jesús García-Colunga; Edwin G Pérez; Angélica Fierro
Journal:  Front Pharmacol       Date:  2018-07-10       Impact factor: 5.810

4.  Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor.

Authors:  Charles L C Smelt; Victoria R Sanders; Joseph Newcombe; Richard P Burt; Tom D Sheppard; Maya Topf; Neil S Millar
Journal:  Neuropharmacology       Date:  2018-07-20       Impact factor: 5.250
  4 in total

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