Nitrone계 항산화제 (PBN)의 뇌에서 혈액으로의 배출과 뇌 수송 특성

• 영문명: Characterization of the Brain Transport and Brain-to-Blood Efflux of Nitrone Based Antioxidant, PBN
• 발행기관: 대한약학회
• 저자명: 이나영(Na-Young Lee) 강영숙(Young-Sook Kang)
• 간행물 정보: 『약학회지』제47권 제4호 (2003년), 224~229쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2003.08.30

영문 초록

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.

키워드

blood-brain barrier a-pheny1-n-tert-buty1 nitrone choline transporter conditionally immortalized rat brain capillary endothelial cell line efflux transport.