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Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates |
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| Authors: | Dorota ?a?ewska Ma?gorzata Wi?cek Xavier Ligneau Tim Kottke Lilia Weizel Roland Seifert Walter Schunack Holger Stark Katarzyna Kie?-Kononowicz |
| Institution: | 1. Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, ul. Medyczna 9, 30-688 Kraków, Poland;2. Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France;3. Institute of Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Strasse 9, 60438 Frankfurt/Main, Germany;4. Institute of Pharmacology, Medical School of Hannover, Carl-Neuberg-Strasse 1, 30625 Hannover, Germany;5. Institute of Pharmacy, Free University of Berlin, Königin-Luise-Strasse 2+4, 14195 Berlin, Germany |
| Abstract: | A series of imidazole-containing (non-)chiral carbamates were tested at human histamine H3 receptor (H3R). All compounds displayed Ki values below 100 nM. A trend for a stereoselectivity at human H3R was observed for the chiral α-branched ligands. Selected compounds were also tested at human histamine H4 receptor and showed moderate to weak affinities (118–1460 nM). |
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