Abstract
A functional screening highlighted a series of spiro-piperidines as 5-HT2B receptor antagonists. Preliminary structure-activity relationship has been explored driving to potent antagonists (IC50 = 1 nM) and indicating directions for further explorations.
MeSH terms
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Inhibitory Concentration 50
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Ligands
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / pharmacology*
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Receptor, Serotonin, 5-HT2B / metabolism
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Serotonin 5-HT2 Receptor Antagonists*
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Structure-Activity Relationship
Substances
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Ligands
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Piperidines
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Receptor, Serotonin, 5-HT2B
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Serotonin 5-HT2 Receptor Antagonists