Literature DB >> 24365158

Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors.

Zhuang Jin1, Pasha Khan1, Youseung Shin1, Jingyi Wang2, Li Lin1, Michael D Cameron1, Jon M Lindstrom2, Paul J Kenny1, Theodore M Kamenecka3.   

Abstract

The design and synthesis of a series of substituted heteroaromatic α4β2α5 positive allosteric modulators is reported. The optimization and development of the heteroaromatic series was carried out from NS9283, and several potent analogues, such as 3-(5-(pyridin-3-yl)-2H-tetrazol-2-yl)benzonitrile (5k) and 3,3'-(2H-tetrazole-2,5-diyl)dipyridine (12 h) with good in vitro efficacy were discovered.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Positive allosteric modulators; Substituted heteroaromatics; α4β2α5

Mesh：

Substances：

Year:  2013        PMID： 24365158      PMCID： PMC3929235          DOI： 10.1016/j.bmcl.2013.11.049

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


  27 in total

Review 1.  Recent advances in positive allosteric modulators of the AMPA receptor.

Authors:  John A Morrow; John K F Maclean; Craig Jamieson
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2.  Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine.

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Journal:  Nature       Date:  2005-07-07       Impact factor: 49.962

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Authors:  Fahmi Himo; Timothy Lovell; Robert Hilgraf; Vsevolod V Rostovtsev; Louis Noodleman; K Barry Sharpless; Valery V Fokin
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8.  Nicotine activation of alpha4* receptors: sufficient for reward, tolerance, and sensitization.

Authors:  Andrew R Tapper; Sheri L McKinney; Raad Nashmi; Johannes Schwarz; Purnima Deshpande; Cesar Labarca; Paul Whiteaker; Michael J Marks; Allan C Collins; Henry A Lester
Journal:  Science       Date:  2004-11-05       Impact factor: 47.728

9.  Cholinergic nicotinic receptor genes implicated in a nicotine dependence association study targeting 348 candidate genes with 3713 SNPs.

Authors:  Scott F Saccone; Anthony L Hinrichs; Nancy L Saccone; Gary A Chase; Karel Konvicka; Pamela A F Madden; Naomi Breslau; Eric O Johnson; Dorothy Hatsukami; Ovide Pomerleau; Gary E Swan; Alison M Goate; Joni Rutter; Sarah Bertelsen; Louis Fox; Douglas Fugman; Nicholas G Martin; Grant W Montgomery; Jen C Wang; Dennis G Ballinger; John P Rice; Laura Jean Bierut
Journal:  Hum Mol Genet       Date:  2006-11-29       Impact factor: 6.150

Review 10.  The scientific case that nicotine is addictive.

Authors:  I P Stolerman; M J Jarvis
Journal:  Psychopharmacology (Berl)       Date:  1995-01       Impact factor: 4.530
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3.  An Accessory Agonist Binding Site Promotes Activation of α4β2* Nicotinic Acetylcholine Receptors.

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Journal:  J Biol Chem       Date:  2015-04-13       Impact factor: 5.157

4.  Promoting activity of (α4)3(β2)2 nicotinic cholinergic receptors reduces ethanol consumption.

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5.  α2-Null mutant mice have altered levels of neuronal activity in restricted midbrain and limbic brain regions during nicotine withdrawal as demonstrated by cfos expression.

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  6 in total

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