Abstract
For the development of novel 5-HT(4) receptor ligands we have designed and synthesized two series of 5-methoxytryptamine derivatives varying the substitution on the primary amine. Their biological activities were evaluated in a receptor binding assay where a subset of compounds showed comparable potency to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses have highlighted promising avenues for further synthetic work and binding modes were proposed by docking these compounds into a homology model of the 5-HT(4) receptor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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5-Methoxytryptamine / analogs & derivatives
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5-Methoxytryptamine / chemical synthesis
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5-Methoxytryptamine / metabolism
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5-Methoxytryptamine / pharmacology
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Animals
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COS Cells
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Chlorocebus aethiops
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Drug Design
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Drug Discovery
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Humans
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Ligands
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Receptors, Serotonin, 5-HT4 / metabolism
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Receptors, Serotonin, 5-HT4 / physiology
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Serotonin 5-HT4 Receptor Antagonists / chemical synthesis*
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Serotonin 5-HT4 Receptor Antagonists / pharmacology*
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Tryptamines / agonists
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Tryptamines / chemical synthesis
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Tryptamines / chemistry
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Tryptamines / pharmacology*
Substances
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Ligands
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Serotonin 5-HT4 Receptor Antagonists
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Tryptamines
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Receptors, Serotonin, 5-HT4
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5-Methoxytryptamine