Huang, Guozheng and Pemp, Daniela and Stadtmueller, Patricia and Nimczick, Martin and Heilmann, Joerg and Decker, Michael (2014) Design, synthesis and in vitro evaluation of novel uni- and bivalent ligands for the cannabinoid receptor type 1 with variation of spacer length and structure. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 24 (17). pp. 4209-4214. ISSN 0960-894X, 1464-3405
Full text not available from this repository. (Request a copy)Abstract
Using rimonabant, a potent inverse agonist for cannabinoid receptor type 1 (CB1R), as parent ligand, a series of novel univalent and bivalent ligands were designed by variation of spacer length and its chemical structure. The ligands synthesized were evaluated for affinity and selectivity by radioligand displacement and a functional steady-state GTPase assay. The results showed the nature of the spacer influences the biological readout. Albeit all compounds show significantly lower affinities than rimonabant, this fact could be used to demonstrate that affinities and selectivity are influenced by the chemical structure and length of the spacer and might be helpful for designing bivalent probes for other GPCR receptors. (C) 2014 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PHARMACOLOGICAL-PROPERTIES; BIOLOGICAL EVALUATION; POTENT; STRATEGIES; AGONISTS; Bivalent ligand; Cannabinoid receptor; CB1; Rimonabant |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Aug 2019 09:13 |
| Last Modified: | 28 Aug 2019 09:13 |
| URI: | https://pred.uni-regensburg.de/id/eprint/9661 |
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