Otaplimastat

Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor -mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury In Vitro Otaplimastat (87.5-350 μM; 20 min) protects neuronal cells against NMDA-induced cell death in a competitive manner. Otaplimastat (350 μM) inhibits Ca 2+ influx following activation of NMDA receptors in primary cultured neuron. Otaplimastat (2-200 μM; pretreated for 4 h) significantly suppresses H 2 O 2 -induced cell death and reactive oxygen species production. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Otaplimastat (10-20 mg/kg; i.p. 30 min before occlusion and 1 h after reperfusion) prevents ischemic neuronal death in the occlusion model of MCA . Otaplimastat (5-10 mg/kg; i.p. daily for 10 days) attenuates impairment of stroke-induced motor function. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (280-310 g, 9 weeks) were induced transient middle cerebral artery (MCA) occlusion Dosage: 10, 20 mg/kg Administration: I.p. before 30 min and after an hour of the MCA-occlusion operation Result: Significantly reduced infarct volume. Improved spatial learning and memory impairments. IC50& Target:MMP NMDA

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