| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363353 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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 δ/μ antagonists, as determined by the functional [S35]GTPγS binding assay, the dimerization of potent Aia-based ‘parent’ ligands unexpectedly resulted in substantial less efficient receptor binding and non-active dimeric compounds.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Steven Ballet, Ewa D. Marczak, Debby Feytens, Severo Salvadori, Yusuke Sasaki, Andrew D. Abell, Lawrence H. Lazarus, Gianfranco Balboni, Dirk Tourwé,