- N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
Bioorganic & medicinal chemistry letters (2004-09-03)
Ian Egle, Nancy Barriault, Michel Bordeleau, Jillian Drage, Laurence Dube, Jack Peragine, Lucy Mazzocco, Jalaj Arora, Keith Jarvie, Ashok Tehim
PMID15341937
摘要
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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