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In vivo Brain-to-blood Efflux Transport of Choline at the Blood-brain Barrier  

Lee Na-Young (College of Pharmacy, Sookmyung Women's University)
Kang Young-Sook (College of Pharmacy, Sookmyung Women's University)
Publication Information
Biomolecules & Therapeutics / v.14, no.1, 2006 , pp. 45-49 More about this Journal
Abstract
The purpose of this study was to clarify the efflux transport system of choline from brain to blood across the blood-brain barrier (BBB) in rats using the brain efflux index (BEI) method. $[^3H]$Choline was micro-injected into parietal cortex area 2 (Par2) of the rat brain, and was eliminated from the brain with elimination halflife of 45 min. The BBB efflux clearance of $[^3H]$choline was about 124 mL/min/g brain, which was determined from combination of an elimination rate constant $(1.54X10^{-2}min^{-1})$ and the distribution volume in the brain (8.05 mL/g brain). The efflux of $[^3H]$choline was inhibited by unlabeled choline in a dose-dependent manner and was significantly inhibited by cationic substrates, such as hemicholinium-3 and tetraethylammonium (TEA). These results suggest that the BBB may act as an efflux pump for choline to reduce the excessive choline concentration in the brain interstitial fluid.
Keywords
Blood-brain barrier; Choline; Efflux transport;
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