Abstract
A series of novel aporphine derivatives were synthesized for initial screening at the 5-HT(2) receptor subtypes. Among them, Compounds 11a and 11b were identified as potent 5-HT(2C) hit ligands with high selectivity over other 5-HT(2) receptor subtypes. Molecular docking study revealed that compounds 11a and 11b formed two key interactions with the binding site of 5-HT(2C) receptor, including a salt-bridge to D3.32 and a H-bond interaction with N6.55.