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Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors |
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| Authors: | Kueny-Stotz Marie Chassaing Stefan Brouillard Raymond Nielsen Mogens Goeldner Maurice |
| Affiliation: | aLaboratoire de Chimie des Polyphénols, UMR 7177 CNRS, Institut Le Bel, 4, rue Blaise Pascal, Université Louis Pasteur Strasbourg, F-67008 Strasbourg, France;bLaboratoire de Chimie Bioorganique, UMR 7175 CNRS, Faculté de Pharmacie, Université Louis Pasteur Strasbourg, 74 route du Rhin, F-67401 Illkirch, France;cUniversity of Copenhagen, Faculty of Pharmaceutical Sciences, 2 Universitetsparken, 2100 Copenhagen, DK, Denmark |
| Abstract: | The synthesis of a series of derivatized flavylium cations was undertaken and the affinity to the benzodiazepine binding site of the GABA-A receptor evaluated. The observed high affinity for some derivatives (sub-μM range) was explained by an in vitro transformation of the flavylium cations into the corresponding trans-retrochalcones, components which are proposed to be the active species in this series. |
| Keywords: | Benzodiazepine binding site Chalcones |
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