Literature DB >> 19560354

Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.

Scott R Breining1, Merouane Bencherif, Sharon R Grady, Paul Whiteaker, Michael J Marks, Charles R Wageman, Henry A Lester, Daniel Yohannes.   

Abstract

Direct comparison of pyridine versus pyrimidine substituents on a small but diverse set of ligands indicates that the pyrimidine substitution has the potential to enhance affinity and/or functional activity at alpha6 subunit-containing neuronal nicotinic receptors (NNRs) and decrease activation of ganglionic nicotinic receptors, depending on the scaffold. The ramifications of this structure-activity relationship are discussed in the context of the design of small molecules targeting smoking cessation.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19560354      PMCID： PMC6107347          DOI： 10.1016/j.bmcl.2009.05.085

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


  30 in total

1.  The subunit composition and pharmacology of alpha-Conotoxin MII-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay.

Authors:  Outi Salminen; Paul Whiteaker; Sharon R Grady; Allan C Collins; J Michael McIntosh; Michael J Marks
Journal:  Neuropharmacology       Date:  2005-04       Impact factor: 5.250

2.  Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras.

Authors:  Roger L Papke; Linda P Dwoskin; Peter A Crooks; Guangrong Zheng; Zhenfa Zhang; J Michael McIntosh; Clare Stokes
Journal:  Neuropharmacology       Date:  2008-03-28       Impact factor: 5.250

3.  Human alpha6 AChR subtypes: subunit composition, assembly, and pharmacological responses.

Authors:  A Kuryatov; F Olale; J Cooper; C Choi; J Lindstrom
Journal:  Neuropharmacology       Date:  2000-10       Impact factor: 5.250

4.  Introduction of unsaturation into the N-n-alkyl chain of the nicotinic receptor antagonists, NONI and NDNI: effect on affinity and selectivity.

Authors:  Sangeetha P Sumithran; Peter A Crooks; Rui Xu; Jun Zhu; Agripina G Deaciuc; Lincoln H Wilkins; Linda P Dwoskin
Journal:  AAPS J       Date:  2005-08-29       Impact factor: 4.009

5.  Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.

Authors:  Jotham W Coe; Paige R Brooks; Michael G Vetelino; Michael C Wirtz; Eric P Arnold; Jianhua Huang; Steven B Sands; Thomas I Davis; Lorraine A Lebel; Carol B Fox; Alka Shrikhande; James H Heym; Eric Schaeffer; Hans Rollema; Yi Lu; Robert S Mansbach; Leslie K Chambers; Charles C Rovetti; David W Schulz; F David Tingley; Brian T O'Neill
Journal:  J Med Chem       Date:  2005-05-19       Impact factor: 7.446

6.  Functional responses and subunit composition of presynaptic nicotinic receptor subtypes explored using the novel agonist 5-iodo-A-85380.

Authors:  Adrian J Mogg; Francis A Jones; Ian A Pullar; Christopher G V Sharples; Susan Wonnacott
Journal:  Neuropharmacology       Date:  2004-11       Impact factor: 5.250

Review 7.  Multiple brain pathways and receptors underlying tobacco addiction.

Authors:  Jed E Rose
Journal:  Biochem Pharmacol       Date:  2007-08-03       Impact factor: 5.858

8.  Rodent habenulo-interpeduncular pathway expresses a large variety of uncommon nAChR subtypes, but only the alpha3beta4* and alpha3beta3beta4* subtypes mediate acetylcholine release.

Authors:  Sharon R Grady; Milena Moretti; Michele Zoli; Michael J Marks; Alessio Zanardi; Luca Pucci; Francesco Clementi; Cecilia Gotti
Journal:  J Neurosci       Date:  2009-02-18       Impact factor: 6.167

9.  Subunit composition and pharmacology of two classes of striatal presynaptic nicotinic acetylcholine receptors mediating dopamine release in mice.

Authors:  Outi Salminen; Karen L Murphy; J Michael McIntosh; John Drago; Michael J Marks; Allan C Collins; Sharon R Grady
Journal:  Mol Pharmacol       Date:  2004-06       Impact factor: 4.436

10.  Pharmacology of alpha-conotoxin MII-sensitive subtypes of nicotinic acetylcholine receptors isolated by breeding of null mutant mice.

Authors:  Outi Salminen; Jennifer A Drapeau; J Michael McIntosh; Allan C Collins; Michael J Marks; Sharon R Grady
Journal:  Mol Pharmacol       Date:  2007-03-06       Impact factor: 4.436
View more
  6 in total

Review 1.  Progress and challenges in the study of α6-containing nicotinic acetylcholine receptors.

Authors:  Sharon R Letchworth; Paul Whiteaker
Journal:  Biochem Pharmacol       Date:  2011-06-28       Impact factor: 5.858

2.  In vitro and in vivo neuronal nicotinic receptor properties of (+)- and (-)-pyrido[3,4]homotropane [(+)- and (-)-PHT]: (+)-PHT is a potent and selective full agonist at α6β2 containing neuronal nicotinic acetylcholine receptors.

Authors:  F Ivy Carroll; Hernán A Navarro; S Wayne Mascarella; Ana H Castro; Charles W Luetje; Charles R Wageman; Michael J Marks; Asti Jackson; M Imad Damaj
Journal:  ACS Chem Neurosci       Date:  2015-04-30       Impact factor: 4.418

3.  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

4.  A novel α-conotoxin MII-sensitive nicotinic acetylcholine receptor modulates [(3) H]-GABA release in the superficial layers of the mouse superior colliculus.

Authors:  Tristan D McClure-Begley; Charles R Wageman; Sharon R Grady; Michael J Marks; J Michael McIntosh; Allan C Collins; Paul Whiteaker
Journal:  J Neurochem       Date:  2012-05-09       Impact factor: 5.372

5.  TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors.

Authors:  Teagan R Wall; Brandon J Henderson; George Voren; Charles R Wageman; Purnima Deshpande; Bruce N Cohen; Sharon R Grady; Michael J Marks; Daniel Yohannes; Paul J Kenny; Merouane Bencherif; Henry A Lester
Journal:  Front Pharmacol       Date:  2017-09-26       Impact factor: 5.810

6.  Analysis of rare variations reveals roles of amino acid residues in the N-terminal extracellular domain of nicotinic acetylcholine receptor (nAChR) alpha6 subunit in the functional expression of human alpha6*-nAChRs.

Authors:  Bhagirathi Dash; Ming D Li
Journal:  Mol Brain       Date:  2014-05-02       Impact factor: 4.041
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.