Sepimostatdimethanesulfonate(FUT-187)通过拮抗NR2BN-methyl-D-aspartate受体发挥神经保护作用，作用位点在NR2B亚基的Ifenprodil结合位点。Sepimostatdimethanesulfonate抑制Ifenprodil结合的Ki值为27.7 µM。
Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM[1].
Sepimostat (1 to 100 nmol/eye, intravitreal injection) exhibits significant neuroprotective effect[1]. Animal Model: Male Sprague Dawley rats weighing 150-300 g[1].
[1]. Masahiro Fuwa, et al. Nafamostat and Sepimostat Identified as Novel Neuroprotective Agents via NR2B N-methyl-D-aspartate Receptor Antagonism Using a Rat Retinal Excitotoxicity Model. Sci Rep. 2019 Dec 31;9(1):20409.
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