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Cerestat is an NMDA receptor antagonist (IC50 = 36 nM).1 It is selective for the NMDA receptor over sigma receptors (IC50 = 2,540 nM). Cerestat (1 mg/kg) reduces infarct volume and the number of steps and errors in a foot fault test in a rat model of stroke induced by middle cerebral artery occlusion.2 It also reduces cortical and striatal neuronal necrosis in a rat model of temporary focal ischemia when administered at a dose of 1.13 mg/kg.3
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1. Synthesis and structure-
2. Effects of cerestat and NBQX on functional and morphological outcomes in rat focal cerebral ischemia. Pharmacol. Biochem. Behav. 68(3), 443-447 (2000).
3. The N-