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2 rezultati
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.
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We synthesized several novel 2-O- or 11-O-substituted N-alkylnoraporphines and assessed their affinities at dopamine D(1) and D(2), and serotonin 5-HT(1A) receptors in rat forebrain tissue. Tested compounds displayed moderate to high affinities to D(2) receptors but low affinities to D(1) and
Receptor-based pharmacophores for serotonin 5-HT7R antagonists-implications to selectivity.
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A set of 31 diversified 5-HT7 receptor antagonists was automatically docked to a conformational ensemble of rhodopsin-based 5-HT7R models (flexible docking). It was found that ergolines, aporphines, and tricyclic psychotropic agents were always docked in a pocket formed by TMHs 4-6, and besides the
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