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Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series |
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| Authors: | Labeeuw Olivier Levoin Nicolas Poupardin-Olivier Olivia Calmels Thierry Ligneau Xavier Berrebi-Bertrand Isabelle Robert Philippe Lecomte Jeanne-Marie Schwartz Jean-Charles Capet Marc |
| Institution: | Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France. o.labeeuw@bioprojet.com |
| Abstract: | 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. |
| Keywords: | Histamine Histamine H3 receptor GPCR hERG |
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