A series of N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D4 (hD4) and 5-HT2A receptors. Several compounds displayed selectivity for these receptors versus hD2 and α1 adrenergic receptors of over 500-fold.

A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure–activity relationships studied. Potent ligands selective for human D4 (hD4) over hD2 and α1 have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC50 of 1500nM.