Bioorganic and Medicinal Chemistry Letters 2004-Nov
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.
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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.