Abstract
New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT(2C) receptor agonists. Appropriate substitution of the amino group (R(1)R(2)N-) gave compounds that were potent 5-HT(2C) agonists with minimal activation of the 5-HT(2A) and 5-HT(2B) receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.
MeSH terms
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Animals
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Benzazepines / chemical synthesis*
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Benzazepines / chemistry
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Benzazepines / pharmacokinetics*
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Humans
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Mice
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Receptor, Serotonin, 5-HT2C / metabolism
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Serotonin 5-HT2 Receptor Agonists*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacokinetics*
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Swiss 3T3 Cells
Substances
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Benzazepines
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Receptor, Serotonin, 5-HT2C
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Serotonin 5-HT2 Receptor Agonists
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Sulfonamides