Schneider, Erich and Mayer, Matthias and Ziemek, Ralf and Li, antao Li and Hutzler, Christoph and Bernhardt, Guenther and Buschauer, Armin (2006) A simple and powerful flow cytometric method for the simultaneous determination of multiple parameters at g protein-coupled receptor subtypes. CHEMBIOCHEM, 7 (9). pp. 1400-1409. ISSN 1439-4227,
Full text not available from this repository. (Request a copy)Abstract
The quantification of pharmacological parameters at G protein-coupled receptors (GPCRs) is indispensable in drug research but costly and time-consuming when conventional methods are sequentially applied. With neuropeptide Y (NPY) Y-1, Y-2, and Y-5 receptors as model systems, a homogenous flow cytometric method for the simultaneous determination of the affinity, selectivity, and activity of GPCR ligands was developed. Mixtures of cells expressing the receptors of interest and cyonine-labeled NPY as a universal fluorescent Y-1, Y-2, and Y-5 receptor agonist were used. Calcium mobilization was measured in different channels with the aid of fluo-4 and fura red A combination of dye-loaded HEL-Y, and CHO-Y-2-G alpha(qi5) cells with unloaded HEC-1B-Y-5 cells allowed the simultaneous determination of Y-1, Y-2, and Y-5 receptor selectivity preceded by the Y-1 and Y-2 receptor-mediated response with one and the some sample. The data are in good agreement with those determined by radioligand binding and spectro fluorimetry. The convenient, robust, and inexpensive multiparametric procedure offers a broad range of applications in the pharmacological characterization of GPCR ligands.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | FLUORESCENCE CORRELATION SPECTROSCOPY; CELLS; LIGANDS; BINDING; LYMPHOCYTE; EXPRESSION; DYES; Y-1; binding affinity; calcium mobilization; flow cytometry; fluorescent probes; receptors |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 01 Feb 2021 10:51 |
| Last Modified: | 01 Feb 2021 10:51 |
| URI: | https://pred.uni-regensburg.de/id/eprint/34057 |
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