Abstract
2,3-Dihydro-1,4-benzodioxanes with aryl 8-aza-bicyclo[3.2.1]oct-3-ene attachments 2 produce compounds with potent 5-HT-T affinity, and weak 5-HT(1A) affinity and alpha(1) affinity. This compares with 2,3-dihydro-1,4-benzodioxanes containing 8-aza-bicyclo[3.2.1] octan-3-ol attachments 4 which possess potent 5-HT(1A) affinity, moderate to good selectivity over alpha(1) and little 5-HT-T affinity. A 3-benzothiophene analogue of 4 (30) was synthesized which possesses potent 5-HT(1A) affinity and especially good selectivity over both alpha(1) and 5-HT-T.
MeSH terms
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Bridged Bicyclo Compounds / metabolism
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Bridged Bicyclo Compounds / pharmacology*
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Dioxanes / metabolism
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Dioxanes / pharmacology*
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Humans
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Octanes / metabolism
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Octanes / pharmacology*
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Receptor, Serotonin, 5-HT1A / metabolism
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Selective Serotonin Reuptake Inhibitors / metabolism
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin 5-HT1 Receptor Antagonists*
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Serotonin Antagonists / metabolism
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Serotonin Antagonists / pharmacology*
Substances
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Bridged Bicyclo Compounds
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Dioxanes
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Octanes
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Serotonin 5-HT1 Receptor Antagonists
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Serotonin Antagonists
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Serotonin Uptake Inhibitors
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Receptor, Serotonin, 5-HT1A