Rose J M, Audus K L
Department of Pharmaceutical Chemistry, University of Kansas, School of Pharmacy, Lawrence 66047, USA.
Peptides. 1998;19(6):1023-30. doi: 10.1016/s0196-9781(98)00054-0.
Angiotensin II (Ang II) uptake and transport across monolayers of bovine brain microvessel endothelial cells (BMECs) was demonstrated. Ang II transport was linear up to 2 h, saturable with a K(m) of 1.7 nM, and tended to be polarized with the apical-to-basolateral transport being greater. [3H]Ang II transport was found to be inhibited by excess unlabeled Ang II, by the Ang II analog sarathrin, and by the endocytic inhibitor phenylarsine oxide. Ang II-(2-8) and-(3-8) were shown to significantly increase the transport of Ang II. These results demonstrate for the first time the receptor-mediated transcytosis of Ang II across brain microvessel endothelium.
已证实血管紧张素II（Ang II）可被牛脑微血管内皮细胞（BMECs）单层摄取并转运。Ang II的转运在长达2小时内呈线性，具有1.7 nM的米氏常数（K(m)）可饱和，并且倾向于极化，从顶端到基底外侧的转运更大。发现[3H]Ang II的转运受到过量未标记的Ang II、Ang II类似物沙拉新以及内吞抑制剂苯砷氧化物的抑制。已表明Ang II-(2-8)和-(3-8)可显著增加Ang II的转运。这些结果首次证明了Ang II通过脑微血管内皮的受体介导的转胞吞作用。
