Document Detail


Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter.
MedLine Citation:
PMID:  20462759     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Guangrong Zheng; Zhenfa Zhang; Paul R Lockman; Werner J Geldenhuys; David D Allen; Linda P Dwoskin; Peter A Crooks
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2010-04-24
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-05-21     Completed Date:  2010-08-10     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3208-10     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Blood-Brain Barrier*
Ligands
Membrane Transport Proteins / metabolism*
Quaternary Ammonium Compounds / metabolism*
Salts
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
U19 DA017548/DA/NIDA NIH HHS
Chemical
Reg. No./Substance:
0/Ligands; 0/Membrane Transport Proteins; 0/Quaternary Ammonium Compounds; 0/Salts; 0/choline transporter

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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