Keller, Max and Schindler, Lisa and Bernhardt, Guenther and Buschauer, Armin (2015) Toward Labeled Argininamide-Type NPY Y-1 Receptor Antagonists: Identification of a Favorable Propionylation Site in BIBO3304. ARCHIV DER PHARMAZIE, 348 (6). pp. 390-398. ISSN 0365-6233, 1521-4184
Full text not available from this repository. (Request a copy)Abstract
Aiming at molecular tools for the neuropeptide Y Y-1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (i) propionylation at the guanidine group (3), (ii) substitution at the urea moiety with a propionamidobutyl residue (4), and (iii) replacement of ureidomethyl by a propionylaminomethyl group (5). With K-i and K-b values in the range of 1.5-4.3nM, determined in binding and functional assays, and high selectivity for the Y1R over the Y2R, Y4R, and Y5R, compounds 4 and 5 were identified as promising candidates for radiolabeling by [H-3]propionylation according to established protocols.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NEUROPEPTIDE-Y; HIGHLY POTENT; AFFINITY; CANCER; LUMINESCENCE; RADIOLIGAND; SUBTYPES; LIGANDS; Acylguanidine; Argininamide; BIBO3304; Neuropeptide Y; NPY Y-1 receptor antagonist |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 15 Jul 2019 07:24 |
| Last Modified: | 15 Jul 2019 07:24 |
| URI: | https://pred.uni-regensburg.de/id/eprint/5420 |
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