Adelaide Research & Scholarship
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https://hdl.handle.net/2440/59847
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| Type: | Journal article |
| Title: | Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds |
| Author: | Ballet, S. Marczak, E. Feytens, D. Salvadori, S. Sasaki, Y. Abell, A. Lazarus, L. Balboni, G. Tourwe, D. |
| Citation: | Bioorganic and Medicinal Chemistry Letters, 2010; 20(5):1610-1613 |
| Publisher: | Pergamon-Elsevier Science Ltd |
| Issue Date: | 2010 |
| ISSN: | 0960-894X 1464-3405 |
| Statement of Responsibility: | Steven Ballet, Ewa D. Marczak, Debby Feytens, Severo Salvadori, Yusuke Sasaki, Andrew D. Abell, Lawrence H. Lazarus, Gianfranco Balboni and Dirk Tourwé |
| Abstract: | The dimerization and trimerization of the Dmt-Tic, Dmt-Aia and Dmt-Aba pharmacophores provided multiple ligands which were evaluated in vitro for opioid receptor binding and functional activity. Whereas the Tic- and Aba multimers proved to be dual and balanced delta/mu antagonists, as determined by the functional [S(35)]GTPgammaS binding assay, the dimerization of potent Aia-based 'parent' ligands unexpectedly resulted in substantial less efficient receptor binding and non-active dimeric compounds. |
| Keywords: | Designed multiple ligands Constrained amino acids Dual μ/δ opioid antagonists |
| Rights: | Copyright © 2010 Elsevier Ltd All rights reserved. |
| DOI: | 10.1016/j.bmcl.2010.01.055 |
| Grant ID: | http://purl.org/au-research/grants/arc/20103228 |
| Published version: | http://dx.doi.org/10.1016/j.bmcl.2010.01.055 |
| Appears in Collections: | Aurora harvest Chemistry and Physics publications IPAS publications |
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