Hollis T M, Sill H W, Butler C, Campos M J, Gardner T W
Department of Biology, Mueller Laboratory, Pennsylvania State University, University Park 16802.
J Diabetes Complications. 1992 Oct-Dec;6(4):230-5. doi: 10.1016/1056-8727(92)90057-r.
We examined the potential of astemizole, a histamine H1-receptor antagonist that does not cross the blood-brain barrier, to reverse blood-retinal barrier leakage to albumin in streptozotocin diabetic rats. Four groups of nondiabetic and four groups of diabetic rats received vehicle or astemizole at dosages of 5, 10, or 20 mg/kg body weight for days 22-28 of a 28-day holding period. There were no significant differences in nondiabetic plasma-vitreous albumin ratios between animals receiving vehicle or any of the three astemizole dosages. Only diabetic rats receiving vehicle showed a significant (p < 0.05) 100% increase in the plasma-vitreous albumin ratio over their nondiabetic counterparts. Diabetic rats receiving either 5, 10, or 20 mg/kg astemizole exhibited total normalization of vitreous albumin accumulation, despite persistence of diabetes. These data indicate that astemizole, an H1-receptor antagonist that does not cross the blood-retinal barrier, is effective in reversing blood-retinal barrier leakage of albumin in experimental diabetes.
我们研究了阿司咪唑（一种不穿过血脑屏障的组胺H1受体拮抗剂）逆转链脲佐菌素诱导的糖尿病大鼠血视网膜屏障对白蛋白渗漏的可能性。四组非糖尿病大鼠和四组糖尿病大鼠在28天饲养期的第22 - 28天接受溶剂对照或剂量为5、10或20 mg/kg体重的阿司咪唑。接受溶剂对照或三种阿司咪唑剂量中任何一种的非糖尿病动物的血浆 - 玻璃体白蛋白比率无显著差异。只有接受溶剂对照的糖尿病大鼠的血浆 - 玻璃体白蛋白比率比其非糖尿病对应物显著增加（p < 0.05）100%。接受5、10或20 mg/kg阿司咪唑的糖尿病大鼠尽管糖尿病持续存在，但玻璃体白蛋白积累完全恢复正常。这些数据表明，阿司咪唑这种不穿过血视网膜屏障的H1受体拮抗剂在实验性糖尿病中可有效逆转血视网膜屏障对白蛋白的渗漏。
