Terawaki T, Takakuwa T, Iguchi S, Wakitani K, Kira H, Okegawa T, Kawasaki A, Masuda Y
Minase Research Institute, Ono Pharmaceutical Co., Ltd., Osaka, Japan.
Eur J Pharmacol. 1988 Jul 26;152(1-2):63-70. doi: 10.1016/0014-2999(88)90836-9.
We evaluated the inhibitory activity of a novel prostacyclin analog, OP-2507 (15-cis-(4-n-propylcyclohexyl)-16,17,18,19,20-pentanor-9-deo xy-6,9 alpha- nitriloprostaglandin F1 methyl ester) on the brain edema induced by occlusion of the middle cerebral artery in cats. Middle cerebral artery occlusion for 4h caused a decrease of regional cerebral blood flow. The specific gravity of the cerebral cortex measured 4h after the middle cerebral artery occlusion as an index of cerebral edema showed a significant reduction. Intravenous infusion of OP-2507 at infusion rates of 10 and 50 ng/kg per min was started 30 min before the middle cerebral artery occlusion and was continued for 4.5 h. While OP-2507 did not affect the blood pressure, heart rate and regional cerebral blood flow before and after the middle cerebral artery occlusion, the reduction of the specific gravity of cerebral cortex was significantly prevented by OP-2507 treatment at both doses. Prostacyclin prevented the reduction of the specific gravity only at the higher dose of 50 ng/kg per min. The present results indicate the potential usefulness of OP-2507 in acute ischemic cerebral disorders.
我们评估了一种新型前列环素类似物OP - 2507（15 - 顺式 -（4 - 正丙基环己基）- 16,17,18,19,20 - 五降 - 9 - 脱氧 - 6,9α - 腈基前列腺素F1甲酯）对猫大脑中动脉闭塞所致脑水肿的抑制活性。大脑中动脉闭塞4小时导致局部脑血流量减少。大脑中动脉闭塞4小时后测量的大脑皮质比重作为脑水肿指标显示显著降低。在大脑中动脉闭塞前30分钟开始以每分钟10和50纳克/千克的输注速率静脉输注OP - 2507，并持续4.5小时。虽然OP - 2507在大脑中动脉闭塞前后不影响血压、心率和局部脑血流量，但两种剂量的OP - 2507治疗均显著阻止了大脑皮质比重的降低。前列环素仅在较高剂量每分钟50纳克/千克时阻止了比重的降低。目前的结果表明OP - 2507在急性缺血性脑疾病中具有潜在的应用价值。
