5-HT7 Receptor Antagonists with an Unprecedented Selectivity Profile.

Ali Ates, Pierre Burssens, Olivier Lorthioir, Patrick Lo Brutto, Gwenael Dehon, Jean Keyaerts, Francis Coloretti,Bénédicte Lallemand,Valérie Verbois,Michel Gillard,Céline Vermeiren

CHEMMEDCHEM（2018）

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摘要

Selective leads: In this study, we generated a new series of serotonin 5-HT7 receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT7 antagonists with unprecedented high selectivity for the 5-HT7 receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.

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关键词

5-HT7 receptor, antagonists, selectivity, serotonin

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