Biselli, Sabrina and Alencastre, Ines and Tropmann, Katharina and Erdmann, Daniela and Chen, Mengya and Littmann, Timo and Maia, Andre F. and Gomez-Lazaro, Maria and Tanaka, Miho and Ozawa, Takeaki and Keller, Max and Lamghari, Meriem and Buschauer, Armin and Bernhardt, Guenther (2020) Fluorescent H-2 Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications. ACS MEDICINAL CHEMISTRY LETTERS, 11 (8). pp. 1521-1528. ISSN 1948-5875,
Full text not available from this repository. (Request a copy)Abstract
Fluorescence labeled ligands have been gaining importance as molecular tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hH(2)R, a series of squaramides labeled with pyridinium or cyanine fluorophores (19-27) was synthesized and characterized. The highest hH(2)R affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists 19-21 (pK(i): 7.71-7.76) and cyanine labeled antagonists 23 and 25 (pK(i): 7.67, 7.11). These fluorescent ligands proved to be useful tools for binding studies (saturation and competition binding as well as kinetic experiments), using confocal microscopy, flow cytometry, and high content imaging. Saturation binding experiments revealed pK(d) values comparable to the pK(i) values. The fluorescent probes 21, 23, and 25 could be used to localize H-2 receptors in HEK cells and to determine the binding affinities of unlabeled compounds.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HISTAMINE H-2-RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; AUTORADIOGRAPHIC LOCALIZATION; CYCLIC-AMP; LIGANDS; DERIVATIVES; BINDING; Histamine H-2 receptor; squaramides; fluorescence labeling; flow cytometry; high content imaging; confocal microscopy |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 16 Mar 2021 08:25 |
| Last Modified: | 16 Mar 2021 08:25 |
| URI: | https://pred.uni-regensburg.de/id/eprint/44022 |
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