DR 2313 是一种选择性，竞争性的和可透过血脑屏障的PARP抑制剂，对PARP-1和PARP-2的IC50值分别为 0.20 和 0.24 μM。它在体内外均有对缺血性损伤的神经保护作用。

DR 2313 is a competitive inhibitor of poly(ADP-ribose) polymerase (IC50: 0.20 and 0.24 μM for PARP-1 and PARP-2 respectively). It also has neuroprotective.

DR 2313 decreases neuronal cell death in models of cerebral ischemia in vivo and in vitro.

In both permanent and transient focal ischemia models in rats, pretreatment with DR2313 (10 mg/kg i.v. bolus and 10 mg/kg/h i.v. infusion for 6 h) significantly reduced the cortical infarct volume.?To determine the therapeutic time window of neuroprotection by DR2313, the effect of post-treatment was examined in transient focal ischemia model and compared with that of a free radical scavenger, MCI-186 (3-methyl-1-phenyl-2-pyrazolone-5-one).?Pretreatment with MCI-186 (3 mg/kg i.v. bolus and 3 mg/kg/h i.v. infusion for 6 h) significantly reduced the infarct volume, whereas the post-treatment failed to show any effects.?In contrast, post-treatment with DR2313 (same regimen) delaying for 2 h after ischemia still prevented the progression of infarction.?These results indicate that DR2313 exerts neuroprotective effects via its potent PARP inhibition, even when the treatment is initiated after ischemia.?Thus, a PARP inhibitor like DR2313 may be more useful in treating acute stroke than a free radical scavenger[1].

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C8H10N2OS

182.24

DR 2313

DMSO:83.3mg/mL
H2O:9.1mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years