Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT_2C receptor.

ABSTRACT: A series of novel aporphine derivatives were synthesized for initial screening at the 5-HT₂ receptor subtypes. Among them, Compounds 11a and 11b were identified as potent 5-HT_2C hit ligands with high selectivity over other 5-HT₂ 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.

SUBMITTER: Xu Y 

PROVIDER: S-EPMC11492304 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature