Abstract
The understanding of the physiological role of the G-protein coupled serotonin 5-HT(7) receptor is largely rudimentary. Therefore, selective and potent pharmacological tools will add to the understanding of serotonergic effects mediated through this receptor. In this report, we describe two compound classes, chromans and tetralins, encompassing compounds with nanomolar affinity for the 5-HT(7) receptor and with good selectivity. Within theses classes, we have discovered both agonists and antagonists that can be used for further understanding of the pharmacology of the 5-HT(7) receptor.
MeSH terms
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Animals
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CHO Cells
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Chromans / chemical synthesis*
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Chromans / chemistry
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Chromans / pharmacology
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Cricetinae
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Cyclic AMP / biosynthesis
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Ligands
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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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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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / chemistry
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Serotonin Receptor Agonists / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Tetrahydronaphthalenes / chemical synthesis*
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Tetrahydronaphthalenes / chemistry
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Tetrahydronaphthalenes / pharmacology
Substances
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Chromans
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Ligands
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Receptors, Serotonin
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Serotonin Antagonists
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Serotonin Receptor Agonists
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Tetrahydronaphthalenes
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serotonin 7 receptor
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Cyclic AMP