Literature DB >> 20979364

Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.

Nurulain Zaveri1, Faming Jiang, Cris Olsen, Willma Polgar, Lawrence Toll.   

Abstract

Antagonist activity at the α3β4 nicotinic acetylcholine receptor (nAChR) is thought to contribute to the antiaddictive properties of several compounds. However, truly selective ligands for the α3β4 nAChR have not been available. We report the discovery and SAR of a novel class of compounds that bind to the α3β4 nAChR and have no measurable affinity for the α4β2 or α7 subtype. In functional assays the lead compound antagonized epibatidine-induced Ca(2+) flux in α3β4-transfected cells in a noncompetitive manner.

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Year:  2010        PMID： 20979364      PMCID： PMC2997436          DOI： 10.1021/jm1006148

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  38 in total

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Journal:  Curr Drug Targets CNS Neurol Disord       Date:  2002-08

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Journal:  J Med Chem       Date:  2003-06-19       Impact factor: 7.446

4.  Measuring nicotinic receptors with characteristics of alpha4beta2, alpha3beta2 and alpha3beta4 subtypes in rat tissues by autoradiography.

Authors:  David C Perry; Yingxian Xiao; Henry N Nguyen; John L Musachio; Martha I Dávila-García; Kenneth J Kellar
Journal:  J Neurochem       Date:  2002-08       Impact factor: 5.372

5.  Antagonism of alpha 3 beta 4 nicotinic receptors as a strategy to reduce opioid and stimulant self-administration.

Authors:  Stanley D Glick; Isabelle M Maisonneuve; Barbara A Kitchen; Mark W Fleck
Journal:  Eur J Pharmacol       Date:  2002-03-01       Impact factor: 4.432

6.  Analysis of mecamylamine stereoisomers on human nicotinic receptor subtypes.

Authors:  R L Papke; P R Sanberg; R D Shytle
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7.  18-MC reduces methamphetamine and nicotine self-administration in rats.

Authors:  S D Glick; I M Maisonneuve; H A Dickinson
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8.  Mecamylamine, dihydro-beta-erythroidine, and dextromethorphan block conditioned responding evoked by the conditional stimulus effects of nicotine.

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Journal:  Pharmacol Biochem Behav       Date:  2009-09-22       Impact factor: 3.533

9.  Modulation of nicotine self-administration in rats by combination therapy with agents blocking alpha 3 beta 4 nicotinic receptors.

Authors:  Stanley D Glick; Isabelle M Maisonneuve; Barbara A Kitchen
Journal:  Eur J Pharmacol       Date:  2002-07-19       Impact factor: 4.432

10.  Membrane potential fluorescence: a rapid and highly sensitive assay for nicotinic receptor channel function.

Authors:  Richard W Fitch; Yingxian Xiao; Kenneth J Kellar; John W Daly
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  22 in total

1.  AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats.

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Journal:  Neuropsychopharmacology       Date:  2012-01-25       Impact factor: 7.853

2.  Medial habenula output circuit mediated by α5 nicotinic receptor-expressing GABAergic neurons in the interpeduncular nucleus.

Authors:  Yun-Wei A Hsu; Lynne Tempest; Lely A Quina; Aguan D Wei; Hongkui Zeng; Eric E Turner
Journal:  J Neurosci       Date:  2013-11-13       Impact factor: 6.167

3.  The α3β4* nicotinic ACh receptor subtype mediates physical dependence to morphine: mouse and human studies.

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Journal:  Br J Pharmacol       Date:  2014-08       Impact factor: 8.739

4.  A Simple Representation of Three-Dimensional Molecular Structure.

Authors:  Seth D Axen; Xi-Ping Huang; Elena L Cáceres; Leo Gendelev; Bryan L Roth; Michael J Keiser
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Review 5.  Cholinergic System and Its Therapeutic Importance in Inflammation and Autoimmunity.

Authors:  Namrita Halder; Girdhari Lal
Journal:  Front Immunol       Date:  2021-04-15       Impact factor: 7.561

6.  Pharmacological stress is required for the anti-alcohol effect of the α3β4* nAChR partial agonist AT-1001.

Authors:  Andrea Cippitelli; Gloria Brunori; Kelly A Gaiolini; Nurulain T Zaveri; Lawrence Toll
Journal:  Neuropharmacology       Date:  2015-02-14       Impact factor: 5.250

7.  Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.

Authors:  Yafei Jin; Xiaoqin Huang; Roger L Papke; Emily M Jutkiewicz; Hollis D Showalter; Chang-Guo Zhan
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8.  High affinity α3β4 nicotinic acetylcholine receptor ligands AT-1001 and AT-1012 attenuate cocaine-induced conditioned place preference and behavioral sensitization in mice.

Authors:  Taline V Khroyan; Dennis Yasuda; Lawrence Toll; Willma E Polgar; Nurulain T Zaveri
Journal:  Biochem Pharmacol       Date:  2015-08-07       Impact factor: 5.858

9.  Activation of GABAergic neurons in the interpeduncular nucleus triggers physical nicotine withdrawal symptoms.

Authors:  Rubing Zhao-Shea; Liwang Liu; Xueyan Pang; Paul D Gardner; Andrew R Tapper
Journal:  Curr Biol       Date:  2013-11-14       Impact factor: 10.834

10.  Differential expression and function of nicotinic acetylcholine receptors in subdivisions of medial habenula.

Authors:  Pei-Yu Shih; Staci E Engle; Gyeon Oh; Purnima Deshpande; Nyssa L Puskar; Henry A Lester; Ryan M Drenan
Journal:  J Neurosci       Date:  2014-07-16       Impact factor: 6.167
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