ME-3277

Rabbits (2-3 kg) induced by photochemical reaction^[1]

0.15, 0.3, and 0.6 mg/kg bolus, followed by 0.125, 0.25, and 0.5 mg/kg/h infusion

i.v., 30 min post-photochemical reaction for 24 h

Inhibited ex vivo platelet aggregation significantly and maintained through the 24-hour period, with inhibition ratios of approximately 60, 80, and 90% at low, middle, and high doses, respectively.
Prolonged bleeding time at 2 or 24 hours after the photochemical reaction but by less than 2-fold at low dose.
Significantly prolonged the bleeding time by about 3-fold at both 2 hours and 24 hours at high dose.
Increased the total reflow time in a dose-dependent manner.
Significantly increased the total reflow time (31.7% vs. 3.8% in vehicle) and had a tendency to improve the 24 hours patency at high dose.
Significantly decreased the neurologic score to 3.5 at a low dose, 4.5 at a middle dose, and 3.5 at a high dose, respectively.
Decreased the infarct volume of total and cerebral cortex area to 13.1% and 4.7% at a low dose, 16.4% and 7.1% at a middle dose, and 12.9% and 5.2% at a high dose, respectively.
Significantly decreased the hemorrhagic volume.
The hemorrhage volume normalized to infarct volume did not differ significantly among the treatment groups and the vehicle control group.