What question did this study set out to answer?

The aim is to discover and evaluate new N-arylindole derivatives as selective GluN2B-NMDAR antagonists for treating ischemic stroke with reduced cardiotoxicity.

March 13, 2026

Discovery and Evaluation of N-Arylindole-Based GluN2B-NMDAR Antagonists with Reduced Cardiotoxicity for the Treatment of Ischemic Stroke.

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Authors

ZZZhuo ZhangShenyang Pharmaceutical University KDKe DuChina Medical University ZLZhenlu LiuShenyang Pharmaceutical University

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Implication

Novel N-arylindole candidate demonstrates neuroprotection in ischemic stroke, suggesting a safer therapeutic option.

Key Points

The aim is to discover and evaluate new N-arylindole derivatives as selective GluN2B-NMDAR antagonists for treating ischemic stroke with reduced cardiotoxicity.
Developed and characterized NFI23, an N-arylindole derivative.
Conducted molecular docking and competitive binding assays.
Assessed neuroprotection through in vitro testing and rat MCAO model.
Evaluated pharmacokinetics, including absorption and brain penetration.
Analyzed receptor interactions and cardiotoxicity liabilities.
NFI23 demonstrated low nanomolar affinity for GluN2B-NMDAR.
It effectively reduced calcium influx and reactive oxygen species generation.
In vivo tests showed significant neuroprotection in the rat MCAO model.
NFI23 preserved mitochondrial membrane potential and p-ERK1/2 expression levels.
Negligible hERG channel inhibition indicated lower cardiotoxicity risk.

Cite This Study

Zhang et al. (2026) studied this question.

synapsesocial.com/papers/69b3ab5e02a1e69014ccc225 https://doi.org/10.1021/acs.jmedchem.5c03741

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Discovery and Evaluation of N-Arylindole-Based GluN2B-NMDAR Antagonists with Reduced Cardiotoxicity for the Treatment of Ischemic Stroke.

Discussion

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Implication

Key Points

Cite This Study

Discovery and Evaluation of N-Arylindole-Based GluN2B-NMDAR Antagonists with Reduced Cardiotoxicity for the Treatment of Ischemic Stroke.

Discussion

Member takes

Implication

Key Points

Cite This Study

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