Szczepanska, Katarzyna and Karcz, Tadeusz and Dichiara, Maria and Mogilski, Szczepan and Kalinowska-Tluscik, Justyna and Pilarski, Boguslaw and Leniak, Arkadiusz and Pietrus, Wojciech and Podlewska, Sabina and Popiolek-Barczyk, Katarzyna and Humphrys, Laura J. and Ruiz-Cantero, M. Carmen and Reiner-Link, David and Leitzbach, Luisa and Lazewska, Dorota and Pockes, Steffen and Gorka, Michal and Zmyslowski, Adam and Calmels, Thierry and Cobos, Enrique J. and Marrazzo, Agostino and Stark, Holger and Bojarski, Andrzej J. and Amata, Emanuele and Kiec-Kononowicz, Katarzyna (2023) Dual Piperidine-Based Histamine H<sub>3</sub> and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain. JOURNAL OF MEDICINAL CHEMISTRY, 66 (14). pp. 9658-9683. ISSN 0022-2623, 1520-4804
Full text not available from this repository. (Request a copy)Abstract
In search of new dual-acting histamine H-3/sigma-1receptorligands, we designed a series of compounds structurally based on highlyactive in vivo ligands previously studied and describedby our team. However, we kept in mind that within the previous series,a pair of closely related compounds, KSK67 and KSK68, differing only in the piperazine/piperidine moietyin the structural core showed a significantly different affinity atsigma-1 receptors (& sigma;(1)Rs). Therefore, we first focusedon an in-depth analysis of the protonation states of piperazine andpiperidine derivatives in the studied compounds. In a series of 16new ligands, mainly based on the piperidine core, we selected threelead structures (3, 7, and 12) for further biological evaluation. Compound 12 showeda broad spectrum of analgesic activity in both nociceptive and neuropathicpain models based on the novel molecular mechanism.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | FORMALIN INJECTION; MOUSE MODELS; PROTEIN; DOCKING; DERIVATIVES; RAT; ANTAGONISTS; AGONIST; CHOLINESTERASE; GENERATION; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 09 Apr 2024 09:50 |
| Last Modified: | 09 Apr 2024 09:50 |
| URI: | https://pred.uni-regensburg.de/id/eprint/60783 |
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