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9
a Binding experiments on 5-HT1A receptors were realized according to
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receptors but exhibited a relatively good affinity for
5-HT1A receptors. Compounds 16a, and especially 16d,
showed, however, a moderate selectivity towards the
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This difference in pharmacological profiles underlines
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The virtual screening of a chemolibrary allowed us to
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the selected compounds has rapidly led to new ligands
with nanomolar affinity on human 5-HT7 receptors.
Our results confirm that the introduction of a hydrogen
bond acceptor leads to potent compounds with an
antagonist profile as predicted by a molecular modeling
study. The chemical modulations of these structures will
be pursued to establish structure–activity relationships,
to design more potent and more selective compounds
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