New (Nor)Aza-Adamantanes Are Agonists at the Newly Identified Serotonin 5HT4 Receptor and Antagonists at the 5HT3 Receptor

Document Type

Article

Publication Date

12-1-1992

Publication Title

Bioorganic & Medicinal Chemistry Letters

Volume

2

Issue

12

Pages

1613-1618

Publisher Name

Elsevier

Abstract

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.

Comments

Author Posting © Elsevier, 1992. The definitive version was published in Bioorganic & Medicinal Chemistry Letters, Volume 2, Issue 12, December 1992. http://dx.doi.org/10.1016/S0960-894X(00)80441-2

Creative Commons License

Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.

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