Keller, Max and Erdmann, Daniela and Pop, Nathalie and Pluym, Nikola and Teng, Shangjun and Bernhardt, Guenther and Buschauer, Armin (2011) Red-fluorescent argininamide-type NPY Y-1 receptor antagonists as pharmacological tools. BIOORGANIC & MEDICINAL CHEMISTRY, 19 (9). pp. 2859-2878. ISSN 0968-0896, 1464-3391
Full text not available from this repository. (Request a copy)Abstract
Fluorescently labelled NPY Y-1 receptor (Y1R) ligands were synthesized by connecting pyrylium and cyanine dyes with the argininamide-type Y1R antagonist core structure by linkers, covering a wide variety in length and chemical nature, attached to the guanidine group. The most promising fluorescent probes had Y1R affinities (radioligand binding) and antagonistic activities (calcium assay) in the one-to two-digit nanomolar range. These compounds turned out to be stable under assay conditions and to be appropriate for the detection of Y(1)Rs by confocal microscopy in live cells. To improve the signal-to-noise ratio by shifting the emission into the near infrared, a new benzothiazolium-type fluorescent cyanine dye (UR-DE99) was synthesized and attached to the parent antagonist via a carbamoyl linker yielding UR-MK131, a highly potent fluorescent Y1R probe, which was also successfully applied in flow cytometry. (C) 2011 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NEUROPEPTIDE-Y RECEPTORS; SUBTYPE SELECTIVITY; CHAMELEON LABELS; FLOW-CYTOMETRY; HIGHLY POTENT; EXPRESSION; CANCER; AFFINITY; TUMORS; CELLS; NPY Y-1 receptor; Fluorescent ligands; Y1R binding; Y1R antagonism; Argininamide derivatives; Confocal microscopy; Flow cytometry |
| 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: | 22 Jun 2020 04:50 |
| Last Modified: | 22 Jun 2020 04:50 |
| URI: | https://pred.uni-regensburg.de/id/eprint/20886 |
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