Literature DB >> 21397497

Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.

Guangrong Zheng1, Zhenfa Zhang, Cheryl Dowell, Elzbieta Wala, Linda P Dwoskin, Joseph R Holtman, J Michael McIntosh, Peter A Crooks.   

Abstract

A series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary structure-activity relationships of these analogs suggest that increased rigidity in the linker units results in higher potency in inhibition of α9α10 nAChRs and greater selectivity over α7 nAChRs. These analogs represent a new class of analgesic for the treatment of neuropathic and tonic inflammatory pain.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21397497      PMCID： PMC3726002          DOI： 10.1016/j.bmcl.2011.02.043

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


  25 in total

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Authors:  L P Dwoskin; L H Wilkins; J R Pauly; P A Crooks
Journal:  Ann N Y Acad Sci       Date:  1999-04-30       Impact factor: 5.691

2.  A novel human nicotinic receptor subunit, alpha10, that confers functionality to the alpha9-subunit.

Authors:  Frédéric Sgard; Eric Charpantier; Sonia Bertrand; Nancy Walker; Daniel Caput; David Graham; Daniel Bertrand; François Besnard
Journal:  Mol Pharmacol       Date:  2002-01       Impact factor: 4.436

3.  A novel alpha-conotoxin, PeIA, cloned from Conus pergrandis, discriminates between rat alpha9alpha10 and alpha7 nicotinic cholinergic receptors.

Authors:  J Michael McIntosh; Paola V Plazas; Maren Watkins; María E Gomez-Casati; Baldomero M Olivera; A Belén Elgoyhen
Journal:  J Biol Chem       Date:  2005-06-27       Impact factor: 5.157

4.  Molecular evolution of the nicotinic acetylcholine receptor: an example of multigene family in excitable cells.

Authors:  N Le Novère; J P Changeux
Journal:  J Mol Evol       Date:  1995-02       Impact factor: 2.395

5.  alpha10: a determinant of nicotinic cholinergic receptor function in mammalian vestibular and cochlear mechanosensory hair cells.

Authors:  A B Elgoyhen; D E Vetter; E Katz; C V Rothlin; S F Heinemann; J Boulter
Journal:  Proc Natl Acad Sci U S A       Date:  2001-03-06       Impact factor: 11.205

Review 6.  Evolutionary history of the ligand-gated ion-channel superfamily of receptors.

Authors:  M O Ortells; G G Lunt
Journal:  Trends Neurosci       Date:  1995-03       Impact factor: 13.837

7.  bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors.

Authors:  Joshua T Ayers; Linda P Dwoskin; A Gabriela Deaciuc; Vladimir P Grinevich; Jun Zhu; Peter A Crooks
Journal:  Bioorg Med Chem Lett       Date:  2002-11-04       Impact factor: 2.823

8.  N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonist: inhibition of S(-)-nicotine-evoked [(3)H]dopamine overflow from superfused rat striatal slices.

Authors:  Lincoln H Wilkins; Aaron Haubner; Joshua T Ayers; Peter A Crooks; Linda P Dwoskin
Journal:  J Pharmacol Exp Ther       Date:  2002-06       Impact factor: 4.030

9.  N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonists: interaction with alpha4beta2* and alpha7* neuronal nicotinic receptors.

Authors:  Lincoln H Wilkins; Vladimir P Grinevich; Joshua T Ayers; Peter A Crooks; Linda P Dwoskin
Journal:  J Pharmacol Exp Ther       Date:  2003-01       Impact factor: 4.030

10.  N-n-alkylpyridinium analogs, a novel class of nicotinic receptor antagonists: selective inhibition of nicotine-evoked [3H] dopamine overflow from superfused rat striatal slices.

Authors:  Vladimir P Grinevich; Peter A Crooks; Sangeetha P Sumithran; Aaron J Haubner; Joshua T Ayers; Linda P Dwoskin
Journal:  J Pharmacol Exp Ther       Date:  2003-05-23       Impact factor: 4.030
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  19 in total

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Authors:  Layla Azam; J Michael McIntosh
Journal:  J Neurochem       Date:  2012-08-03       Impact factor: 5.372

2.  Novel small molecule α9α10 nicotinic receptor antagonist prevents and reverses chemotherapy-evoked neuropathic pain in rats.

Authors:  Elzbieta P Wala; Peter A Crooks; J Michael McIntosh; Joseph R Holtman
Journal:  Anesth Analg       Date:  2012-05-18       Impact factor: 5.108

3.  Cloning, synthesis, and characterization of αO-conotoxin GeXIVA, a potent α9α10 nicotinic acetylcholine receptor antagonist.

Authors:  Sulan Luo; Dongting Zhangsun; Peta J Harvey; Quentin Kaas; Yong Wu; Xiaopeng Zhu; Yuanyan Hu; Xiaodan Li; Victor I Tsetlin; Sean Christensen; Haylie K Romero; Melissa McIntyre; Cheryl Dowell; James C Baxter; Keith S Elmslie; David J Craik; J Michael McIntosh
Journal:  Proc Natl Acad Sci U S A       Date:  2015-07-13       Impact factor: 11.205

4.  Pain therapeutics from cone snail venoms: From Ziconotide to novel non-opioid pathways.

Authors:  Helena Safavi-Hemami; Shane E Brogan; Baldomero M Olivera
Journal:  J Proteomics       Date:  2018-05-16       Impact factor: 4.044

Review 5.  α9-containing nicotinic acetylcholine receptors and the modulation of pain.

Authors:  Arik J Hone; Denis Servent; J Michael McIntosh
Journal:  Br J Pharmacol       Date:  2017-07-30       Impact factor: 8.739

Review 6.  Nicotinic acetylcholine receptors in neuropathic and inflammatory pain.

Authors:  Arik J Hone; J Michael McIntosh
Journal:  FEBS Lett       Date:  2017-10-27       Impact factor: 4.124

7.  Nicotinic acetylcholine receptors in dorsal root ganglion neurons include the α6β4* subtype.

Authors:  Arik J Hone; Erin L Meyer; Melissa McIntyre; J Michael McIntosh
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8.  From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.

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Journal:  J Med Chem       Date:  2022-07-14       Impact factor: 8.039

9.  Limited efficacy of α-conopeptides, Vc1.1 and RgIA, to inhibit sensory neuron CaV current.

Authors:  Andrew B Wright; Yohei Norimatsu; J Michael McIntosh; Keith S Elmslie
Journal:  eNeuro       Date:  2015 Jan-Feb

10.  A novel inhibitor of α9α10 nicotinic acetylcholine receptors from Conus vexillum delineates a new conotoxin superfamily.

Authors:  Sulan Luo; Sean Christensen; Dongting Zhangsun; Yong Wu; Yuanyan Hu; Xiaopeng Zhu; Sandeep Chhabra; Raymond S Norton; J Michael McIntosh
Journal:  PLoS One       Date:  2013-01-30       Impact factor: 3.240
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