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New (Nor)Aza-Adamantanes Are Agonists At The Newly Identified Serotonin 5ht4 Receptor And Antagonists At The 5ht3 Receptor, Daniel Flynn, Daniel Becker, Dale Spangler, Roger Nosal
New (Nor)Aza-Adamantanes Are Agonists At The Newly Identified Serotonin 5ht4 Receptor And Antagonists At The 5ht3 Receptor, Daniel Flynn, Daniel Becker, Dale Spangler, Roger Nosal
Daniel P. Becker
New aza(nor)adamantanes 1A, 1B, and 1C are described which exhibit properties of both 5-HT4 agonism and 5-HT3 antagonism. In particular, compound 1C [SC-52491], an azanoradamantane, exhibits an EC50 of 51 nM in a functional model of 5-HT4 agonism and potent antagonism, Ki = 1.2 nM, at the 5-HT3receptor.