期刊
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
卷 20, 期 2, 页码 381-386出版社
NATURE PUBLISHING GROUP
DOI: 10.1097/00004647-200002000-00020
关键词
blood-brain barrier; P-glycoprotein; brain uptake; transporters
An in situ mouse brain perfusion model predictive of passive and carrier-mediated transport across the blood-brain barrier (BBB) was developed and applied to mdr1a P-glycoprotein (Pgp)-deficient mice [mdr1a(-/-)]. Cerebral flow was estimated from diazepam uptake. Physical integrity of the BBB was assessed with sucrose/inulin spaces; functional integrity was assessed with glucose uptake, which was: saturable with a K-m of similar to 17 mmol/L and V-max of 310 mmol . 100 g(-1). min(-1). Brain uptake of a Pgp substrate (colchicine) was significantly enhanced (two- to fourfold) in mdr1a(-/-) mice. These data suggest that the model is applicable to elucidating the effects of efflux transporters, including Pgp, on brain uptake.
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