Pregn-5-en-3β-ol and androst-5-en-3β-ol dicarboxylic acid esters as potential therapeutics for NMDA hypofunction: In vitro safety assessment and plasma stability.

Steroids(2019)

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摘要
•In vitro safety evaluation of positive modulators of NMDA receptor.•NMDA receptor positive allosteric modulation as a potential therapeutic strategy.•Hepatotoxicity and mitotoxicity estimation using HepG2 cells.•Caco-2 permeability assay to evaluate intestinal absorption of novel compounds.•Screening of rat and human plasma stability reveals unforeseen stability of C-3 hemiester moiety.
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关键词
Neurosteroid,NMDA receptor hypofunction,Hepatotoxicity,Mitotoxicity,Caco-2 permeability,Plasma stability
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