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Different antagonist binding properties of human and rat histamine H3 receptors |
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| Authors: | Stark H Sippl W Ligneau X Arrang J M Ganellin C R Schwartz J C Schunack W |
| Affiliation: | 1. Department of Drug Development, Gustave-Roussy Cancer Campus, Villejuif, France;2. European Institute of Oncology, Milan, Italy;3. Vall d''Hebron Institute of Oncology (VHIO), Vall d''Hebron University Hospital, Universitat Autònoma de Barcelona, Barcelona, Spain;4. Sage Bionetworks, Fred Hutchinson Cancer Research Center, Seattle;5. Clovis Oncology, Inc., San Francisco;6. Clovis Oncology, Inc., Boulder,USA;7. Clovis Oncology, Inc., Milan, Italy;8. Institut de Recherche International Servier, Suresnes, France;9. Istituto di Ricerche Farmacologiche Mario Negri, Via La Masa, Milan, Italy |
| Abstract: | Different histamine H3-receptor antagonists have been tested in displacement studies at human and rat H3 receptors in stably transfected cells. Based on an actual rhodopsin structure, models for receptor antagonist interaction were developed for receptors of both species. Similarities and discrepancies in binding profiles can be explained, but not quantified by hydrophilic interactions with Asp114 and an important lipophilic binding pocket modified by two nearby amino acids. |
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