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

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 α 1 have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC 50 of 1500 nM.