The
amisulpride derivatives and R enantiomers of
amisulpride disclosed herein, or pharmaceutical compositions thereof, can be used to antagonize
serotonin (e.g., 5-HT2a, 5-HT7) receptors in a subject, alone or in combination with other CNS active agents. The
amisulpride derivatives and R enantiomers of amisulpride or pharmaceutical compositions thereof disclosed herein can be used, alone or in combination with other CNS active agents, for the treatment of one or more conditions responsive to modulation of
serotonin (e.g., 5-HT2a, 5-HT7) receptors in a subject. The amisulpride derivatives and R enantiomers of amisulpride or pharmaceutical compositions thereof disclosed herein can be used, alone or in combination with other CNS active agents, for the treatment of one or more disorders associated with abnormal
serotonin levels in the brain.