Abstract
This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT(3)A receptors in mammalian cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding, Competitive
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Boron Compounds / chemistry
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Cell Line
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Granisetron / analogs & derivatives*
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Granisetron / chemical synthesis
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Granisetron / chemistry
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Granisetron / pharmacology
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Humans
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Magnetic Resonance Spectroscopy
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Radioligand Assay
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Receptors, Serotonin, 5-HT3 / metabolism*
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Serotonin 5-HT3 Receptor Antagonists
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Serotonin Antagonists / chemical synthesis*
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Serotonin Antagonists / chemistry
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Serotonin Antagonists / pharmacology
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Spectrometry, Mass, Electrospray Ionization
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Structure-Activity Relationship
Substances
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4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
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Boron Compounds
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Receptors, Serotonin, 5-HT3
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Serotonin 5-HT3 Receptor Antagonists
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Serotonin Antagonists
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Granisetron