New (Nor)Aza-Adamantanes Are Agonists at the Newly Identified Serotonin 5HT4 Receptor and Antagonists at the 5HT3 Receptor
Bioorganic & Medicinal Chemistry Letters
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.
Flynn, Daniel L.; Becker, Daniel; Spangler, Dale P.; and Nosal, Roger. New (Nor)Aza-Adamantanes Are Agonists at the Newly Identified Serotonin 5HT4 Receptor and Antagonists at the 5HT3 Receptor. Bioorganic & Medicinal Chemistry Letters, 2, 12: , 1992. Retrieved from Loyola eCommons, Chemistry: Faculty Publications and Other Works, http://dx.doi.org/10.1016/S0960-894X(00)80441-2
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© 1992 Elsevier