Licostinel

• CAT Number: M101751
• CAS Number: 153504-81-5
• Molecular Formula: C8H3Cl2N3O4
• Molecular Weight: 276.03
• Purity: ≥95%
• Synonyms: 6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione
• InChI: InChI=1S/C8H3Cl2N3O4/c9-2-1-3-5(6(4(2)10)13(16)17)12-8(15)7(14)11-3/h1H,(H,11,14)(H,12,15)
• InChIKey: CHFSOFHQIZKQCR-UHFFFAOYSA-N
• SMILES: C1=C2C(=C(C(=C1Cl)Cl)[N+](=O)[O-])NC(=O)C(=O)N2

Licostinel (CAT: M101751) is a small-molecule compound that functions as a competitive antagonist at the glycine-binding site of the N-methyl-D-aspartate (NMDA) receptor, with a binding affinity (K_b) of 5 nM. This inhibition of NMDA receptor activity was investigated for its potential neuroprotective effects in conditions such as stroke and traumatic brain injury. Despite showing promise in preclinical studies, clinical trials were discontinued due to limited efficacy and the emergence of side effects, including transient sedation, dizziness, and nausea. Additionally, at higher concentrations, Licostinel exhibited antagonistic activity at AMPA and kainate receptors, with K_b values of 0.9 μM and 2.5 μM, respectively.