Characterization of the Brain Transport and Brain-to-Blood Efflux of Nitrone Based Antioxidant, PBN
이나영(Na-Young Lee);강영숙(Young-Sook Kang)
- Abstract
- We have investigated the transport characteristics of synthetic antioxidant and free radical scavenger, α-phe-myl-n-tert-butyl nitrone (PBN) at the blood- brain barrier (BBB) by in vitro uptake study in conditionally immortalized rat brain capillary endothelial cell line (TR-BBB). Also, the efflux of PBN from brain to blood is estimated using the brain efflux index (BEI) Method. Choline is a charged organic cation, including nitrogen-methyl group and shows the carrier-mediated distribution to the brain. [3H]Choline uptake by TR-BBB cells was significantly inhibited by PBN with IC50 of 1.2 mM, which appears to be due to similar structures between choline and PBN. And, PBN was microinjected into Par2 of the rat brain by BEI method, and was eliminated from the brain with an apparent elimination half-life of about 2 min. Also, [3H]choline efflux was significantly inhibited by PBN using BEI method. In conclusion, the efflux transport of PBN takes place across the BBB and PBN may be transported into the brain and eliminated from the brain by BBB choline transporter.
- Keywords : blood-brain barrier;a-pheny1-n-tert-buty1 nitrone;choline transporter;conditionally immortalized rat brain capillary endothelial cell line;efflux transport.
- February 2025, 69 (1)
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