Permeability of porcine blood brain barrier to somatostatin analogues
作者： Gert Fricker , Stephanie Nobmann , David S Miller
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摘要: Transport of a fluorescent somatostatin analogue (NBD-octreotide) across freshly isolated functionally intact capillaries from porcine brain was visualized by confocal microscopy and quantitated image analysis. Luminal accumulation NBD-octreotide showed all characteristics specific energy-dependent transport. Steady-state luminal fluorescence averaged 2 – 3 times cellular reduced to levels when metabolism inhibited NaCN. The in capillary lumens concentration-dependent manner unlabelled octreotide, verapamil, PSC-833 cyclosporin A, potent inhibitors p-glycoprotein, leucotriene C4, strong modulator Mrp2. Conversely, octreotide BODIPY-verapamil on p-glycoprotein fluorescein-methotrexate, None the used significantly substrates. Together, data are consistent with being transported membrane both P-gp Mrp2, providing further evidence that transporters contribute substantially active barrier function this endothelium. British Journal Pharmacology (2002) 135, 1308–1314; doi:10.1038/sj.bjp.0704557
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