Li, L. T. and Mayer, Matthias and Schneider, Erich and Schreiber, Elvira and Bernhardt, Guenther and Peng, S. Q. and Buschauer, Armin (2003) Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A. ARCHIV DER PHARMAZIE, 336 (12). pp. 585-590. ISSN 0365-6233, 1521-4184
Full text not available from this repository. (Request a copy)Abstract
Aspartof a programme to develop fluorescence-based methods for the study of the interactions between G-protein coupled receptors (GPCRs) and their ligands the preparation of low molecular weight fluorescence-labelled neuropeptide Y (NPY)Y-5 antagonists is reported. The naphthylsulfonyl group in the potent quinazoline-type NPYY5 receptor antagonist CGP 71683A was replaced with a dansyl, nitrobenzoxadiazole (NBD) or acridine-9-carbonyl group. In radioligand binding studies on human Y-5 receptor expressing HEC-1B cells the substances labelled with acridine (K-i 311 nM) and NBD (K-i > 1000 nM) proved to be moderately active or inactive, respectively By contrast, a K-i value of 49 nM was found for the dansyl analogue compared to 2 nM for CGP 71683A. No binding to Y-1 receptors (SK-N-MC cells, displacement of [H-3]propionyl-NPY) was detected for the new compounds at concentrations less than or equal to 1 muM.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PHARMACOLOGICAL-ACTIVITY; FOOD-INTAKE; NPY Y-1; CELLS; INTERNALIZATION; neuropeptide Y; Y-5 receptor antagonist; fluorescence labelling; quinazoline; CGP 71683A |
| 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: | 16 Aug 2021 06:37 |
| Last Modified: | 16 Aug 2021 06:37 |
| URI: | https://pred.uni-regensburg.de/id/eprint/38326 |
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