Abstract
The synthesis and pharmacological data of some new and potent hydrophilic 5-HT4 receptor antagonists are described. Propanediol derivative 25 was identified as a potent antagonist with low affinity for the hERG potassium channel and promising pharmacokinetics.
Keywords:
5-HT(4) receptor antagonists; Pharmacokinetic; hERG.
Copyright © 2014. Published by Elsevier Ltd.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Drug Discovery*
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
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Ether-A-Go-Go Potassium Channels / metabolism
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Humans
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Hydrophobic and Hydrophilic Interactions
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Molecular Structure
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Propylene Glycols / chemical synthesis
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Propylene Glycols / chemistry
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Propylene Glycols / pharmacology*
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Receptors, Serotonin, 5-HT4 / metabolism*
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Serotonin 5-HT4 Receptor Antagonists / chemical synthesis
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Serotonin 5-HT4 Receptor Antagonists / chemistry
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Serotonin 5-HT4 Receptor Antagonists / pharmacology*
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Structure-Activity Relationship
Substances
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Ether-A-Go-Go Potassium Channels
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Propylene Glycols
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Serotonin 5-HT4 Receptor Antagonists
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Receptors, Serotonin, 5-HT4