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Licostinel

Names

[ CAS No. ]:
153504-81-5

[ Name ]:
Licostinel

[Synonym ]:
6,7-Dichloro-5-nitro-2,3-quinoxalinedione
Licostinel
5-Nitro-6,7-dichloro-2,3-quinoxalinedione
2,3-Quinoxalinedione,6,7-dichloro-1,4-dihydro-5-nitro
5-nitro-6,7-dichloro-1,4-dihydroquinoxaline-2,3-dione
ACEA-1021
6,7-dichloro-1,4-dihydro-8-nitro-2,3-quinoxalinedione
1,4-dihydro-6,7-dichloro-5-nitroquinoxalin-2,3-dione
6,7-Dichloro-1,4-dihydro-5-nitro-2,3-quinoxalinedione

Biological Activity

[Description]:

Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity[1][2][3].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

59 nM (glycine receptor)[1]


[References]

[1]. Zhou ZL, et al. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Bioorg Med Chem. 2003 Apr 17;11(8):1769-80.  

[2]. Albers GW, et al. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Stroke. 1999 Mar;30(3):508-13.  

[3]. Martin H, et al. Effects of glycine receptor antagonism on spreading depression in the rat. Neurosci Lett. 1994 Oct 24;180(2):285-9.  

Chemical & Physical Properties

[ Density]:
1.757g/cm3

[ Molecular Formula ]:
C8H3Cl2N3O4

[ Molecular Weight ]:
276.03

[ Exact Mass ]:
274.95000

[ PSA ]:
111.54000

[ LogP ]:
1.95460

[ Index of Refraction ]:
1.647

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream