Abstract
A series of 2-alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles were synthesized and evaluated for their 5-HT6 activity. The most potent agonist in this series was 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole with an IC50=7.4 nM in 3H-LSD binding and an EC50=1.0 nM in a functional assay measuring production of cyclic AMP.
MeSH terms
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Cell Line
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Cyclic AMP / biosynthesis
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Humans
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / pharmacology
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Radioligand Assay
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Receptors, Serotonin / chemistry*
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Receptors, Serotonin / metabolism
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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / pharmacology
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Structure-Activity Relationship
Substances
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5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole
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Indoles
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Pyridines
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Receptors, Serotonin
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Serotonin Receptor Agonists
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serotonin 6 receptor
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Cyclic AMP