Lazewska, Dorota and Mogilski, Szczepan and Hagenow, Stefanie and Kuder, Kamil and Gluch-Lutwin, Monika and Siwek, Agata and Wiecek, Malgorzata and Kaleta, Maria and Seibel, Ulla and Buschauer, Armin and Filipek, Barbara and Stark, Holger and Kiec-Kononowicz, Katarzyna (2019) Alkyl derivatives of 1,3,5-triazine as histamine H-4 receptor ligands. BIOORGANIC & MEDICINAL CHEMISTRY, 27 (7). pp. 1254-1262. ISSN 0968-0896, 1464-3391
Full text not available from this repository.Abstract
This study focuses on the design, synthesis, molecular modeling and biological evaluation of a novel group of alkyl-1,3,5-triazinyl-methylpiperazines. New compounds were synthesized and their affinities for human histamine H-4 receptor (hH(4)R) were evaluated. Among them, 4-(cyclohexylmethyl)-6-(4-methylpiperazin-1-yl)1,3,5- triazin-2-amine (14) exhibited hH(4)R affinity with a K-i of 160 nM and behaved as antagonist in functional assays: the cellular aequorin-based assay (IC50= 32 nM) and [S-35] GTP.S binding assay (pKb= 6.67). In addition, antinociceptive activity of 14 in vivo was observed in Formalin test (in mice) and in Carrageenan-induced acute inflammation test (in rats).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NEUROPATHIC PAIN; H4 RECEPTOR; DISCOVERY; H-4-RECEPTOR; JNJ7777120; ACTIVATION; MODELS; Histamine H-4 receptors; Histamine H-4 ligands; 1,3,5-Triazine; Docking; Pain |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 15 Apr 2020 08:06 |
| Last Modified: | 15 Apr 2020 08:06 |
| URI: | https://pred.uni-regensburg.de/id/eprint/27308 |
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