Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

Abstract High-throughput screening of an array of biphenylmethylamines synthesised by high-throughput solid-phase chemistry resulted in the identification of compounds with high-affinity for the 5-ht 5A receptor. The structure–activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11 , a potent and selective 5-ht 5A receptor antagonist.