van Bree J B, Audus K L, Borchardt R T
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence 66045.
Pharm Res. 1988 Jun;5(6):369-71. doi: 10.1023/a:1015959628008.
The mechanism of transport of baclofen, a centrally acting muscle relaxant, across the blood-brain barrier (BBB) was studied using an in vitro model. The model consisted of a monolayer of bovine brain endothelial cells grown in primary culture on a porous regenerated cellulose membrane. The transport of baclofen across the monolayer expressed time and concentration dependency and was saturable. Transport data were corrected for diffusion and fitted to the Michaelis-Menten Vmax model: Km = 58.5 microM, Vmax = 0.23 nmol/min. The results validate the use of the in vitro BBB model as described and support the hypothesis that baclofen penetrates the BBB by means of a carrier-mediated transport system.
使用体外模型研究了中枢性肌肉松弛剂巴氯芬透过血脑屏障（BBB）的机制。该模型由在多孔再生纤维素膜上原代培养的单层牛脑内皮细胞组成。巴氯芬跨单层的转运表现出时间和浓度依赖性且具有饱和性。对转运数据进行扩散校正并拟合到米氏Vmax模型：Km = 58.5微摩尔，Vmax = 0.23纳摩尔/分钟。结果验证了所述体外血脑屏障模型的用途，并支持巴氯芬通过载体介导的转运系统穿透血脑屏障这一假说。
