Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

Herein, we report the synthesis, structure-activity relationship study, and biological evaluation of neurosteroid inhibitors of N-methyl-D-aspartate receptors (NMDARs) receptors that employ an amide structural motif, relative to pregnanolone glutamate (PAG) – a compound with neuroprotective properti...

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Bibliographic Details
Main Authors: Santosh Kumar Adla, Barbora Slavikova, Hana Chodounska, Vojtech Vyklicky, Marek Ladislav, Pavla Hubalkova, Barbora Krausova, Tereza Smejkalova, Michaela Nekardova, Marketa Smidkova, Lenka Monincova, Radko Soucek, Ladislav Vyklicky, Eva Kudova
Format: Article
Language:English
Published: Frontiers Media S.A. 2018-11-01
Series:Frontiers in Pharmacology
Subjects:
neurosteroid
amide
NMDA receptor
plasma stability
structure-activity relationship
Online Access:https://www.frontiersin.org/article/10.3389/fphar.2018.01299/full

Internet

https://www.frontiersin.org/article/10.3389/fphar.2018.01299/full

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