Abstract
Azaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a-d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC-54750 is a potent 5-HT(4) agonist and 5-HT(3) antagonist with in vivo efficacy in gastroparesis models and also inhibits cisplatin-induced emesis.
MeSH terms
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Adamantane / analogs & derivatives*
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Adamantane / chemical synthesis
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Adamantane / chemistry
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Adamantane / pharmacology*
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Animals
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Aza Compounds / chemical synthesis
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Aza Compounds / pharmacology*
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Benzamides / chemical synthesis
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Benzamides / chemistry
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Benzamides / pharmacology*
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Cisplatin / antagonists & inhibitors
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Cisplatin / chemistry
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Dogs
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Gastrointestinal Agents / chemical synthesis
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Gastrointestinal Agents / pharmacology*
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Gastrointestinal Motility / drug effects*
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Rats
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Serotonin 5-HT3 Receptor Antagonists
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Serotonin 5-HT4 Receptor Agonists*
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Serotonin Receptor Agonists / chemical synthesis
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Serotonin Receptor Agonists / pharmacology*
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Vomiting / chemically induced
Substances
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Aza Compounds
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Benzamides
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Gastrointestinal Agents
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SC-52491
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SC-54750
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Serotonin 5-HT3 Receptor Antagonists
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Serotonin 5-HT4 Receptor Agonists
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Serotonin Receptor Agonists
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azaadamantane benzamide
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Adamantane
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Cisplatin