13-05501. Licostinel [Archived]

Nomenclature

CAS number: 153504-81-5
6,7-Dichloro-1,4-dihydro-5-nitro-2,3-quinoxalinedione; 6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione; ACEA-1021.
C8H3Cl2N3O4; mol wt 276.03.
C 34.81%, H 1.10%, Cl 25.69%, N 15.22%, O 23.19%.

Description and references

Antagonist of the NMDA receptor at the glycine site. Prepn: E. Weber, J. F. W. Keana, WO 9400124 (1994); eidem, US 5622952 (1997 to Univ. Oreg; Regents Univ. Calif.); J. F. W. Keana et al., J. Med. Chem. 38, 4367 (1995). Pharmacology in vitro: R. M. Woodward et al., Mol. Pharmacol. 47, 568 (1995); in vivo: B. D. Kretschmer et al., Eur. J. Pharmacol. 331, 109 (1997). Clinical evaluation and pharmacokinetics in acute stroke: G. W. Albers et al., Stroke 30, 508 (1999).

Chemical structure

Properties

Yellow powder, mp 342-344°.

Therapeutic Category

Neuroprotective.

Keywords

Neuroprotective; NMDA Receptor Antagonist

Status

This monograph has been retired and is no longer subject to revision or update.