Wagner, Eva and Wittmann, Hans-Joachim and Elz, Sigurd and Strasser, Andrea (2011) Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21 (21). pp. 6274-6280. ISSN 0960-894X,
Full text not available from this repository. (Request a copy)Abstract
In literature, a synergism between histamine H-1 and H-4 receptor is discussed. Furthermore, it was shown, that the combined application of mepyramine, a H-1 antagonist and JNJ7777120, a H-4 receptor ligand leads to a synergistic effect in the acute murine asthma model. Thus, the aim of this study was to develop new hybrid ligands, containing one H-1 and one H-4 pharmacophor, connected by an appropriate spacer, in order to address both, H1R and H4R. Within this study, we synthesized nine hybrid compounds, which were pharmacologically characterized at hH(1)R and hH(4)R. The new compounds revealed (high) affinity to hH(1)R, but showed only low affinity to hH(4)R. Additionally, we performed molecular dynamic studies for some selected compounds at hH(1)R, in order to obtain information about the binding mode of these compounds on molecular level. (C) 2011 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HISTAMINE H-4 RECEPTOR; PHARMACOLOGICAL HYBRIDS; ANTAGONISTS; HISTAPRODIFENS; SUBSTRUCTURES; H-1-RECEPTOR; INFLAMMATION; ACTIVATION; MECHANISM; BINDING; Histamine H-1 receptor; Histamine H-4 receptor; Mepyramine; JNJ7777120; Hybrid compounds; Molecular dynamics |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 27 May 2020 15:30 |
| Last Modified: | 27 May 2020 15:30 |
| URI: | https://pred.uni-regensburg.de/id/eprint/19926 |
Actions (login required)
 |
View Item |
