Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity.
| Animal Model: | The permanent model of middle cerebral artery occlusion in fisher 344 rats and CD-1 mice. The transient model of focal ischemia in Wistar and Sprague 鈥揇awley rats[2 |
| Dosage: | 5 mg/kg bolus 3.5 mg/kg/h for 6h, 10 mg/kg bolus 7.0 mg/kg/h for 6h |
| Administration: | A single intravenous injection bolus continuous infusion |
| Result: | Decreased infarct size. |
| Animal Model: | Male Sprague-Dawley rats [3] |
| Dosage: | 20, 40, 80 mg/kg for intraperitoneal injection (i.p.) bolus 7 mg/kg/h , 30mins |
| Administration: | Intravenous injection (i.v.) bolus continuous infusion |
| Result: | Reduced the rate of spreading depression and EEG activity in the rat brain in a dose-dependent manner. |
[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.