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Bioorg Med Chem Lett. 2008 Jul 1;18(13):3809-13. doi: 10.1016/j.bmcl.2008.04.081. Epub 2008 May 6.

Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors.

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Institut für Pharmazie, Lehrstuhl für Pharmazeutische/Medizinische Chemie, Friedrich-Schiller-Universität Jena, Philosophenweg 14, 07743 Jena, Germany.


Dibenzo- and benzindolo-azecines represent a novel class of high-affinity dopamine receptor antagonists. To further characterize these drugs as potential neuroleptics, we selected a set of azecine derivatives and ring expanded homologues and we measured their antagonist activity at the 5-HT(2A) receptor in the porcine coronary artery. SARs found for the 5-HT(2A) receptor resemble those for the D1 but not the D2 receptor. The protein-ligand interactions were discussed with respect to the different binding pockets.

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