Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, S Enantiomers Engage Receptors D2 and D3, while R Enantiomers Engage 5-HT7 | Zendy

V. Grattan | Zendy; Andrew R. Vaino | Zendy; Zachary Prensky | Zendy; Mark S. Hixon | Zendy

Open Access

Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, S Enantiomers Engage Receptors D₂ and D₃, while R Enantiomers Engage 5-HT₇

Author(s) -

V. Grattan,

Andrew R. Vaino,

Zachary Prensky,

Mark S. Hixon

Publication year - 2019

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.9b02144

Subject(s) - amisulpride , enantiomer , chemistry , benzamide , antipsychotic , receptor , pharmacology , polypharmacy , atypical antipsychotic , stereochemistry , psychology , biochemistry , psychiatry , medicine , schizophrenia (object oriented programming)

Benzamide antipsychotics such as amisulpride are dosed as racemates though efficacy is assumed to be mediated through S enantiomer binding to D 2 receptors. At prescribed doses, the benzamides likely display polypharmacy since brain exposure should be sufficient to engage the 5-HT 7 receptors, as well. Curiously, the studies herein reveal that racemic dosing is required to engage both targets since the D 2 receptor has an almost 40-fold selectivity for the S enantiomer, while the 5-HT 7 receptor has greater than 50-fold preference for the R enantiomer.

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