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Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750
Daniel P Becker1, Daniel L Flynn, Robert L Shone
1Departments of Medicinal Chemistry and Pharmacology, Pfizer Research & Development, 4901 Searle Parkway, Skokie, IL 60077, USA. dbecke3@luc.edu
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.
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