Literature DB >> 19006672

Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.

Bradley A Scates1, Bethany L Lashbrook, Benjamin C Chastain, Kaoru Tominaga, Brandon T Elliott, Nicholas J Theising, Thomas A Baker, Richard W Fitch.   

Abstract

A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity probes and multivalent ligands for nAChR.

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Year:  2008        PMID: 19006672      PMCID: PMC2903455          DOI: 10.1016/j.bmc.2008.10.045

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  26 in total

1.  Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.

Authors:  N H Lin; Y Li; Y He; M W Holladay; T Kuntzweiler; D J Anderson; J E Campbell; S P Arneric
Journal:  Bioorg Med Chem Lett       Date:  2001-03-12       Impact factor: 2.823

2.  A glia-derived acetylcholine-binding protein that modulates synaptic transmission.

Authors:  A B Smit; N I Syed; D Schaap; J van Minnen; J Klumperman; K S Kits; H Lodder; R C van der Schors; R van Elk; B Sorgedrager; K Brejc; T K Sixma; W P Geraerts
Journal:  Nature       Date:  2001-05-17       Impact factor: 49.962

3.  Nicotinic acetylcholine receptor at 4.6 A resolution: transverse tunnels in the channel wall.

Authors:  A Miyazawa; Y Fujiyoshi; M Stowell; N Unwin
Journal:  J Mol Biol       Date:  1999-05-14       Impact factor: 5.469

4.  Acetylenic pyridines for use in PET imaging of nicotinic receptors.

Authors:  Alan P Kozikowski; Sheela K Chellappan; David Henderson; Roger Fulton; Nicolas Giboureau; Yingxian Xiao; Zhi-Liang Wei; Denis Guilloteau; Patrick Emond; Frederic Dolle; Kenneth J Kellar; Michael Kassiou
Journal:  ChemMedChem       Date:  2007-01       Impact factor: 3.466

5.  Fluorescence techniques for measuring ion channel activity.

Authors:  G Veliçelebi; K A Stauderman; M A Varney; M Akong; S D Hess; E C Johnson
Journal:  Methods Enzymol       Date:  1999       Impact factor: 1.600

6.  Structural and electronic requirements for potent agonists at a nicotinic receptor.

Authors:  C E Spivak; T M Gund; R F Liang; J A Waters
Journal:  Eur J Pharmacol       Date:  1986-01-14       Impact factor: 4.432

7.  Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial.

Authors:  Douglas E Jorenby; J Taylor Hays; Nancy A Rigotti; Salomon Azoulay; Eric J Watsky; Kathryn E Williams; Clare B Billing; Jason Gong; Karen R Reeves
Journal:  JAMA       Date:  2006-07-05       Impact factor: 56.272

Review 8.  Polymer therapeutics: concepts and applications.

Authors:  Rainer Haag; Felix Kratz
Journal:  Angew Chem Int Ed Engl       Date:  2006-02-13       Impact factor: 15.336

9.  Homoepiboxidines: further potent agonists for nicotinic receptors.

Authors:  Richard W Fitch; Xue-Feng Pei; Yumika Kaneko; Tara Gupta; Dan Shi; Irina Federova; John W Daly
Journal:  Bioorg Med Chem       Date:  2004-01-02       Impact factor: 3.641

10.  Schizophrenia and smoking: an epidemiological survey in a state hospital.

Authors:  J de Leon; M Dadvand; C Canuso; A O White; J K Stanilla; G M Simpson
Journal:  Am J Psychiatry       Date:  1995-03       Impact factor: 18.112

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