Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593239 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
The histamine H4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl)quinazolin-2-amine (VUF11489), as a new H4R antagonist. Analysis of its binding kinetics at the human H4R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rogier A. Smits, Herman D. Lim, Tiffany van der Meer, Sebastiaan Kuhne, Karin Bessembinder, Obbe P. Zuiderveld, Maikel Wijtmans, Iwan J.P. de Esch, Rob Leurs,