Literature DB >> 20462759

Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter.

Guangrong Zheng1, Zhenfa Zhang, Paul R Lockman, Werner J Geldenhuys, David D Allen, Linda P Dwoskin, Peter A Crooks.   

Abstract

A series of bis-azaaromatic quaternary ammonium compounds containing flexible polymethylenic linkers as well as conformationally restricted linkers were evaluated for their affinity for the blood-brain barrier choline transporter (BBB-ChT). The preliminary structure-activity relationships obtained from this study suggest that incorporating a linear, conformationally restricted linker into the molecule improves affinity for the BBB-ChT. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20462759      PMCID: PMC3725989          DOI: 10.1016/j.bmcl.2010.04.098

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


  25 in total

1.  Molecular modeling studies on the active binding site of the blood-brain barrier choline transporter.

Authors:  Werner J Geldenhuys; Paul R Lockman; James H McAfee; Kevin T Fitzpatrick; Cornelis J Van der Schyf; David D Allen
Journal:  Bioorg Med Chem Lett       Date:  2004-06-21       Impact factor: 2.823

2.  Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.

Authors:  Peter A Crooks; Joshua T Ayers; Rui Xu; Sangeetha P Sumithran; Vladimir P Grinevich; Lincoln H Wilkins; A Gabriela Deaciuc; David D Allen; Linda P Dwoskin
Journal:  Bioorg Med Chem Lett       Date:  2004-04-19       Impact factor: 2.823

3.  An in situ brain perfusion technique to study cerebrovascular transport in the rat.

Authors:  Y Takasato; S I Rapoport; Q R Smith
Journal:  Am J Physiol       Date:  1984-09

4.  Cation transport specificity at the blood-brain barrier.

Authors:  Paul R Lockman; James H McAfee; Werner J Geldenhuys; David D Allen
Journal:  Neurochem Res       Date:  2004-12       Impact factor: 3.996

5.  Effect of a novel nicotinic receptor antagonist, N,N'-dodecane-1,12-diyl-bis-3-picolinium dibromide, on nicotine self-administration and hyperactivity in rats.

Authors:  N M Neugebauer; Z Zhang; P A Crooks; L P Dwoskin; M T Bardo
Journal:  Psychopharmacology (Berl)       Date:  2005-10-12       Impact factor: 4.530

6.  3D-QSAR study of bis-azaaromatic quaternary ammonium analogs at the blood-brain barrier choline transporter.

Authors:  Werner J Geldenhuys; Paul R Lockman; Tiffany H Nguyen; Cornelis J Van der Schyf; Peter A Crooks; Linda P Dwoskin; David D Allen
Journal:  Bioorg Med Chem       Date:  2005-07-01       Impact factor: 3.641

7.  Active transport of high-affinity choline and nicotine analogs into the central nervous system by the blood-brain barrier choline transporter.

Authors:  David D Allen; Paul R Lockman; Karen E Roder; Linda P Dwoskin; Peter A Crooks
Journal:  J Pharmacol Exp Ther       Date:  2003-03       Impact factor: 4.030

Review 8.  The transport of choline.

Authors:  P R Lockman; D D Allen
Journal:  Drug Dev Ind Pharm       Date:  2002-08       Impact factor: 3.225

Review 9.  Drug and gene targeting to the brain with molecular Trojan horses.

Authors:  William M Pardridge
Journal:  Nat Rev Drug Discov       Date:  2002-02       Impact factor: 84.694

Review 10.  The blood-brain barrier choline transporter as a brain drug delivery vector.

Authors:  D D Allen; P R Lockman
Journal:  Life Sci       Date:  2003-08-15       Impact factor: 5.037

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  5 in total

Review 1.  Transendothelial Transport and Its Role in Therapeutics.

Authors:  Ravi Kant Upadhyay
Journal:  Int Sch Res Notices       Date:  2014-08-27

Review 2.  Nicotinic receptor antagonists as treatments for nicotine abuse.

Authors:  Peter A Crooks; Michael T Bardo; Linda P Dwoskin
Journal:  Adv Pharmacol       Date:  2014

Review 3.  Molecular determinants of blood-brain barrier permeation.

Authors:  Werner J Geldenhuys; Afroz S Mohammad; Chris E Adkins; Paul R Lockman
Journal:  Ther Deliv       Date:  2015-08-25

4.  In silico predictive model to determine vector-mediated transport properties for the blood-brain barrier choline transporter.

Authors:  Sergey Shityakov; Carola Förster
Journal:  Adv Appl Bioinform Chem       Date:  2014-09-02

5.  The yjdF riboswitch candidate regulates gene expression by binding diverse azaaromatic compounds.

Authors:  Sanshu Li; Xue Ying Hwang; Shira Stav; Ronald R Breaker
Journal:  RNA       Date:  2016-02-03       Impact factor: 4.942

  5 in total

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