ArticleScientific reports2017
NMDA receptor antagonism with novel indolyl, 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-malonaldehyde, reduces seizures duration in a rat model of epilepsy.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Integrative Analysis of Trace Elements, Oxidative Stress, and Psychological Distress in Epilepsy: Biochemical Profiling and In Silico Docking Insights.Neurochemical research · 2026Article
- Targeting NMDA Receptor Complex in Management of Epilepsy.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Indoleninyl-substituted pyrimido[1,2-RSC advances · 2021Article
- Cell-Based High-Throughput Screening Protocol for Discovering Antiviral Inhibitors Against SARS-COV-2 Main Protease (3CLpro).Molecular biotechnology · 2021Article
- Pathological Targets for Treating Temporal Lobe Epilepsy: Discoveries From Microscale to Macroscale.Frontiers in neurology · 2021Review
- Dynamic Change of Shanks Gene mRNA Expression and DNA Methylation in Epileptic Rat Model and Human Patients.Molecular neurobiology · 2020Article
- Plasma Exosomal MiRNAs Expression Profile in Mesial Temporal Lobe Epilepsy With Hippocampal Sclerosis: Case-Control Study and Analysis of Potential Functions.Frontiers in molecular neuroscience · 2020Article
- Role of Grina/Nmdara1 in the Central Nervous System Diseases.Current neuropharmacology · 2020Review
- D-Serine Contributes to Seizure Development via ERK Signaling.Frontiers in neuroscience · 2019Article
- Recent developments on triazole nucleus in anticonvulsant compounds: a review.Journal of enzyme inhibition and medicinal chemistry · 2018Review
- Brain Lipopolysaccharide Preconditioning-Induced Gene Reprogramming Mediates a Tolerance State in Electroconvulsive Shock Model of Epilepsy.Frontiers in pharmacology · 2018Article
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Authors and funding
7 authors.
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Abstract
N-methyl-D-aspartate receptors (NMDAR) play a central role in epileptogensis and NMDAR antagonists have been shown to have antiepileptic effects in animals and humans. Despite significant progress in the development of antiepileptic therapies over the previous 3 decades, a need still exists for novel therapies. We screened an in-house library of small molecules targeting the NMDA receptor. A novel indolyl compound, 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-malonaldehyde, (DDBM) showed the best binding with the NMDA receptor and computational docking data showed that DDBM antagonised the binding sites of the NMDA receptor at lower docking energies compared to other molecules. Using a rat electroconvulsive shock (ECS) model of epilepsy we showed that DDBM decreased seizure duration and improved the histological outcomes. Our data show for the first time that indolyls like DDBM have robust anticonvulsive activity and have the potential to be developed as novel anticonvulsants.
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