Document Detail


Novel and highly potent histamine H3 receptor ligands. Part 2: Exploring the cyclohexylamine-based series.
MedLine Citation:
PMID:  21783360     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Synthesis and biological evaluation of novel and potent cyclohexylamine-based histamine H3 receptor inverse agonists are described. Compounds in this newly identified series exhibited subnanomolar binding affinities for human receptor and no significant interaction with hERG channel. One derivative (10t) demonstrated enhanced in vivo efficiency and preferential brain distribution, both properties suitable for potential clinical evaluation.
Authors:
Olivier Labeeuw; Nicolas Levoin; Olivia Poupardin-Olivier; Thierry Calmels; Xavier Ligneau; Isabelle Berrebi-Bertrand; Philippe Robert; Jeanne-Marie Lecomte; Jean-Charles Schwartz; Marc Capet
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-28
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-7-25     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France.
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