Synthesis and Evaluation of a Novel Zuranolone Analog with High GABA<sub>A</sub> Receptor PAM Activity and Excellent Pharmacokinetic Profiles

Synthesis and Evaluation of a Novel Zuranolone Analog with High GABA<sub>A</sub> Receptor PAM Activity and Excellent Pharmacokinetic Profiles

Zuranolone (SAGE-217), the first FDA-approved oral neurosteroid (NAS), a positive allosteric modulator (PAM) of γ-aminobutyric acid type A (GABA<sub>A</sub>) receptor for postpartum depression approved in 2023, has limitations such as short half-life, low bioavailability, and central inh...

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Bibliographic Details
Main Authors: Yingjie Yang, Xu Deng, Hengwei Xu, Daoyuan Chen, Fengjuan Zhao, Huijie Yang, Wenyan Wang, Chunjie Sha, Mingxu Ma, Guanqing Zhang, Liang Ye, Jingwei Tian
Format: Article
Language:English
Published: MDPI AG 2025-04-01
Series:Molecules
Subjects:
Zuranolone analog
neurosteroid (NAS)
GABA<sub>A</sub> receptors
positive allosteric modulator (PAM)
lipophilicity
anticonvulsant effect
Online Access:https://www.mdpi.com/1420-3049/30/9/1918
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