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. 2004 Oct 4;14(19):4847-50.
doi: 10.1016/j.bmcl.2004.07.045.

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists

Ian Egle  1 , Nancy Barriault, Michel Bordeleau, Jillian Drage, Laurence Dube, Jack Peragine, Lucy Mazzocco, Jalaj Arora, Keith Jarvie, Ashok Tehim
Affiliations

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists

Ian Egle et al. Bioorg Med Chem Lett. .

Abstract

A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D(4) (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC(50) of 1500 nM.

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