Li, Liantao and Kracht, Julia and Peng, Shiqi and Bernhardt, Günther and Buschauer, Armin (2003) Synthesis and pharmacological activity of fluorescent histamine H-1 receptor antagonists related to mepyramine. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 13 (7). pp. 1245-1248. ISSN 0960-894X
Full text not available from this repository.Abstract
Fluorescently labeled histamine H-1 receptor antagonists were synthesized starting from N-demethylmepyramine by introduction of omega-aminoalkyl chains (2-8 methylene groups in length) followed by derivatization of the terminal NH2 group with various fluorophores (fluorescein, naphthofluorescein, rhodamine, tetramethylrhodamine, BODIPY, dansyl, and nitrobenzoxadiazole (NBD)). On the isolated guinea pig ileum and in a Ca2+ assay on U373MG human glioblastoma cells the highest H-1 antagonistic activities were found in 5- and 6-carboxyfluorescein labeled compounds with hexa- and octamethylene spacers and in an analogous NBD-aminohexanoyl derivative (pA(2) or pK(B) values in the range: 8.3-9.0; compared to 9.3-9.4 for mepyramine). (C) 2003 Elsevier Science Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | IODOBOLPYRAMINE; LIGANDS; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 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: | 17 Aug 2021 11:18 |
| Last Modified: | 17 Aug 2021 11:18 |
| URI: | https://pred.uni-regensburg.de/id/eprint/39129 |
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