Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, Enantiomers Engage Receptors D and D, while Enantiomers Engage 5-HT.

Benzamide antipsychotics such as amisulpride are dosed as racemates though efficacy is assumed to be mediated through enantiomer binding to D receptors. At prescribed doses, the benzamides likely display polypharmacy since brain exposure should be sufficient to engage the 5-HT receptors, as well. Curiously, the studies herein reveal that racemic dosing is required to engage both targets since the D receptor has an almost 40-fold selectivity for the enantiomer, while the 5-HT receptor has greater than 50-fold preference for the enantiomer.