Department of Neurosurgery, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030, USA.
J Pharmacol Exp Ther. 2011 May;337(2):451-6. doi: 10.1124/jpet.110.176602. Epub 2011 Jan 26.
Darbepoetin alfa (darbEpo) is an erythropoietic glycoprotein that activates the erythropoietin receptor. The aim of our study was to determine whether darbEpo is neuroprotective in a cortical impact injury (CII) model and to determine the characteristics of dose response and time window. To better understand the vascular mechanism of darbEpo neuroprotection, the reactivity of cerebral blood flow (CBF) to l-arginine administration was also studied. Rats were given saline or darbEpo from 2.5 to 50 μg/kg at 5 min after CII or a dose of 25 μg/kg darbEpo at times ranging from 5 min to 24 h after CII. Histological assessment was determined 2 weeks after a severe CII. Other rats were given either darbEpo (25 μg/kg) or saline daily for 3 days before injury. Five minutes after severe CII, they were given either l-arginine or d-arginine. Hemodynamic variables were monitored for 2 h after injury. In the dose-response study, darbEpo in doses of 25 and 50 μg/kg significantly reduced contusion volume from 39.1 ± 6.7 to 8.1 ± 3.1 and 11.2 ± 6.0 mm(3), respectively. In the time window study, darbEpo reduced contusion volume when given in a dose of 25 μg/kg at 5 min to 6 h after the impact injury. In animals pretreated with darbEpo, the CBF response to l-arginine was significantly greater than in the animals pretreated with saline. These data demonstrate that darbEpo has neuroprotective effects in traumatic brain injury in a dose- and time-dependent manner and that vascular effects of darbEpo may have a role in neuroprotection.
达贝泊汀α(darbepoetin alfa,darbEpo)是一种促红细胞生成素糖蛋白,可激活促红细胞生成素受体。本研究旨在确定达贝泊汀在皮质撞击伤(cortical impact injury,CII)模型中是否具有神经保护作用,并确定剂量反应和时间窗的特征。为了更好地了解达贝泊汀神经保护的血管机制,还研究了脑血流(cerebral blood flow,CBF)对 l-精氨酸给药的反应性。大鼠在 CII 后 5 分钟内给予生理盐水或达贝泊汀 2.5 至 50μg/kg,或在 CII 后 5 分钟至 24 小时内给予 25μg/kg 达贝泊汀。严重 CII 后 2 周进行组织学评估。其他大鼠在损伤前每天给予达贝泊汀(25μg/kg)或生理盐水,共 3 天。严重 CII 后 5 分钟,给予 l-精氨酸或 d-精氨酸。损伤后 2 小时监测血流动力学变量。在剂量反应研究中,25μg/kg 和 50μg/kg 的达贝泊汀可使挫伤体积分别从 39.1±6.7mm3减少至 8.1±3.1mm3和 11.2±6.0mm3。在时间窗研究中,25μg/kg 的达贝泊汀在损伤后 5 分钟至 6 小时给予时可减少挫伤体积。在预先用达贝泊汀处理的动物中,l-精氨酸引起的 CBF 反应明显大于预先用生理盐水处理的动物。这些数据表明,达贝泊汀以剂量和时间依赖的方式对创伤性脑损伤具有神经保护作用,并且达贝泊汀的血管作用可能在神经保护中起作用。