Licostinel

Licostinel
Clinical data
Other names	ACEA-1021
ATC code	None;
Identifiers
	IUPAC name 6,7-Dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione;
CAS Number	153504-81-5;
PubChem CID	5486198;
ChemSpider	4588899;
UNII	3Z3037LJTC;
CompTox Dashboard (EPA)	DTXSID60165346 ;
Chemical and physical data
Formula	C8H3Cl2N3O4
Molar mass	276.03 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c1c2c(c(c(c1Cl)Cl)[N+](=O)[O-])[nH]c(=O)c(=O)[nH]2;
	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); Key:CHFSOFHQIZKQCR-UHFFFAOYSA-N;

Licostinel (INN; development code ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (K_b = 5 nM).^[1]^[2]^[3] It was under investigation by Acea Pharmaceuticals as a neuroprotective agent for the treatment of cerebral ischemia associated with stroke and head injuries but was ultimately never marketed.^[1]^[2]^[4] In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed.^[4]^[5] In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the AMPA and kainate receptors at high concentrations (K_b = 0.9 μM and 2.5 μM, respectively).^[3]

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