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New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor |
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| Authors: | Daniel L. Flynn Daniel P. Becker Dale P. Spangler Roger Nosal Gary W. Gullikson Chafiq Moummi Dai-Chang Yang |
| Affiliation: | a Department of Chemistry Searle Research and Development, Skokie, Illinois 60077 USA b Neurological Diseases Research Searle Research and Development, Skokie, Illinois 60077 USA |
| Abstract: | New aza(nor)adamantanes , , and are described which exhibit properties of both 5-HT4 agonism and 5-HT3 antagonism. In particular, compound [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-HT3 receptor. |
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