New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor

doi:10.1016/S0960-894X(00)80441-2

Bioorganic & Medicinal Chemistry Letters

Volume 2, Issue 12, December 1992, Pages 1613-1618

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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-HT₃ receptor.

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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

Abstract

Mol. Pharmacol.

J. Pharmacol. Exp. Ther.

Naunyn-Schmeideberg's Arch. Pharmacol.

J. Org. Chem.