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L-4-chlorokynurenine · AV-101

Small molecule · Antagonist of NMDA receptor glycine-coagonist site (GRIN1) · developed by VistaGen Therapeutics

Phase 2 Most advanced trial (none active)
VTGN Developer
2 Registered trials

What is L-4-chlorokynurenine?

L-4-chlorokynurenine (AV-101) is an orally bioavailable prodrug that crosses the blood-brain barrier and is converted to 7-chlorokynurenic acid, a selective antagonist at the glycine-coagonist site of NMDA receptors. It reduces glutamate excitotoxicity and quinolinic acid synthesis. The drug is studied in Parkinson disease and medication-induced dyskinesia.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as
AV-101
Drug type
Small molecule
Targets
NMDA receptor glycine-coagonist site (GRIN1)
Mechanism
Antagonist of NMDA receptor glycine-coagonist site (GRIN1)
Pathways
NMDA receptor signaling, glutamate excitotoxicity, quinolinic acid synthesis
Therapy area
Neurology
Developer
VistaGen Therapeutics, Inc. (VTGN)
FDA status
Investigational, not approved in the US. Most advanced trial: Phase 2
UNII
77XLH9L40B

🧪 Clinical trials

TrialPhaseConditionStatusSponsor
NCT04147949 Phase 2 Parkinson Disease Unknown VTGN
NCT03583554 Phase 1/2 Healthy Completed VTGN

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Dyskinesia, Medication-InducedHealthyL-Dopa Causing Adverse Effects in Therapeutic UseParkinson Disease

Other drugs acting on GRIN1

More from VistaGen Therapeutics

Sources

Updated Oct 3, 2026. Something wrong or missing? Report it on the VTGN page.

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Data: FDA (Drugs@FDA, Purple Book, DailyMed), NIH (NCI Thesaurus, GSRS, RxNorm), ClinicalTrials.gov • Informational purposes only, not medical or investment advice. • All drugs A–Z

This data is for informational purposes only, not investment advice. BioRadar does not provide buy/sell recommendations. Past performance does not guarantee future results. Always do your own due diligence.