5-HT 7 Receptor Antagonists with an Unprecedented Selectivity Profile

Selective leads: In this study, we generated a new series of serotonin 5-HT receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT antagonists with unprecedented high selectivity for the 5-HT receptor, setting the sta...

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Bibliographic Details
Published inChemMedChem Vol. 13; no. 8; pp. 795 - 802
Main Authors Ates, Ali, Burssens, Pierre, Lorthioir, Olivier, Lo Brutto, Patrick, Dehon, Gwenael, Keyaerts, Jean, Coloretti, Francis, Lallemand, Bénédicte, Verbois, Valérie, Gillard, Michel, Vermeiren, Céline
Format Journal Article
LanguageEnglish
Published Germany 23.04.2018
Subjects
HEK293 Cells
Humans
Isoquinolines - chemistry
Isoquinolines - pharmacology
Receptors, Serotonin - metabolism
Serotonin Antagonists - chemistry
Serotonin Antagonists - pharmacology
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
Structure-Activity Relationship
antagonists
selectivity
5-HT7 receptor
serotonin
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Summary:Selective leads: In this study, we generated a new series of serotonin 5-HT receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT antagonists with unprecedented high selectivity for the 5-HT receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201800026