Keller, Max and Pop, Nathalie and Hutzler, Christoph and Beck-Sickinger, Annette G. and Bernhardt, Guenther and Buschauer, Armin (2008) Guanidine-Acylguanidine Bioisosteric Approach in the Design of Radioligands: Synthesis of a Tritium-Labeled N-G-Propionylargininamide ([H-3]-UR-MK114) as a Highly Potent and Selective Neuropeptide Y Y-1 Receptor Antagonist. JOURNAL OF MEDICINAL CHEMISTRY, 51 (24). pp. 8168-8172. ISSN 0022-2623,
Full text not available from this repository. (Request a copy)Abstract
Synthesis and characterization of (R)-N-alpha-(2,2-diphenylacetyl)-N-(4-hydroxybenzyl)-N-omega-([2,3-H-3]-propanoyl)-argininamide ([H-3]-UR-MK114), an easily accessible tritium-labeled NPY Y-1 receptor (Y1R) antagonist C (K-B: 0.8 nM, calcium assay, HEL cells) derived from the (R)-argininamide BIBP 3226, is reported. The radioligand binds with high affinity (K-D, saturation: 1.2 nM, kinetic experiments: 1.1 nM, SK-N-MC cells) and selectivity for Y1R over Y-2, Y-4, and Y-5 receptors. The title compound is a useful pharmacological tool for the determination of Y1R ligand affinities, quantification of Y1R binding sites, and autoradiography.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NONPEPTIDE ANTAGONIST; PROTECTED GUANIDINES; MC CELLS; CANCER; EXPRESSION; REAGENTS; BIBP3226; BINDING; |
| 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: | 14 Oct 2020 08:22 |
| Last Modified: | 14 Oct 2020 08:22 |
| URI: | https://pred.uni-regensburg.de/id/eprint/29919 |
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