GF120918是一种P-糖蛋白调节剂，可提高大鼠中枢神经系统中未结合的安普那韦浓度。
GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats.
作者信息
Edwards Jeffrey E, Brouwer Kenneth R, McNamara Patrick J
机构信息
Graduate Center for Toxicology, University of Kentucky, Lexington, Kentucky 40536, USA.
出版信息
Antimicrob Agents Chemother. 2002 Jul;46(7):2284-6. doi: 10.1128/AAC.46.7.2284-2286.2002.
Abstract
The goal of this study was to determine the distribution of unbound amprenavir in the central nervous system (CNS) of rats. The concentration of unbound amprenavir in the extracellular fluid of the brain and the blood was examined in the presence and absence of the MDR modulator GF120918 by microdialysis. The brain-to-blood ratio of amprenavir in the absence and presence of GF120918 was found to be significantly different (P < 0.003; 0.076 and 0.617, respectively). The use of the MDR modulator GF120918 could potentially increase the penetration of human immunodeficiency virus protease inhibitors into the CNS.
摘要
本研究的目的是确定安普那韦在大鼠中枢神经系统（CNS）中的游离药物分布情况。通过微透析法，在存在和不存在多药耐药（MDR）调节剂GF120918的情况下，检测了大脑细胞外液和血液中游离安普那韦的浓度。结果发现，在不存在和存在GF120918的情况下，安普那韦的脑血比存在显著差异（P < 0.003；分别为0.076和0.617）。使用MDR调节剂GF120918可能会增加人类免疫缺陷病毒蛋白酶抑制剂进入中枢神经系统的渗透率。
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