KMID : 0606320030190010045
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Journal of Phamacetical Sciences Sookmyung Women s University 2003 Volume.19 No. 1 p.45 ~ p.53
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The Blood-Brain Barrier Permeability and Pharmacokinetics of Ebselen by HPLC Analysis in Rats
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Lee Na-Young
Kang Young-Sook
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Abstract
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Ebselen (2-phenyl-1,2-benzisoselenazol-3(2H)-one) is known to have glutathione peroxidase-like activity and has been proposed as a therapeutic agent for stroke. The purpose of this study was to evaluate the blood-brain barrier (BBB) permeability of ebselen in Sprague-Dawly (SD) rats. The BBB transport and pharmacokinetic parameters of ebselen were investigated in SD rats using single intravenous injection technique. Intact ebselen was removed rapidly with elimination half-life of about 11 min. Brain uptake of ebselen after IV injection at 30 min was 0.11 ¡¾ 0.07%ID/g. Ebselen was transported well to the brain through the BBB in rats, and it is metabolized very rapidly, due to its small molecular size (MW 274) and high lipophilic (log P 2.98) property.
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