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Reservoirs for HIV-1: mechanisms for viral persistence in the presence of antiviral immune responses and antiretroviral therapy.HIV-1储存库：在抗病毒免疫反应和抗逆转录病毒疗法存在的情况下病毒持续存在的机制
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Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.P-糖蛋白转运的药理学抑制增强了HIV-1蛋白酶抑制剂在脑和睾丸中的分布。
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3
Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor.P-糖蛋白对HIV蛋白酶抑制剂安普那韦（141W94）中枢神经系统分布的作用。
Pharm Res. 1999 Aug;16(8):1206-12. doi: 10.1023/a:1018941328702.
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HIV-associated dementia: new insights into disease pathogenesis and therapeutic interventions.HIV相关性痴呆：疾病发病机制与治疗干预的新见解
AIDS Patient Care STDS. 1999 Mar;13(3):153-63. doi: 10.1089/apc.1999.13.153.
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Human immunodeficiency virus protease inhibitors.人类免疫缺陷病毒蛋白酶抑制剂
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Methodological aspects of the use of a calibrator in in vivo microdialysis-further development of the retrodialysis method.体内微透析中校准物使用的方法学方面——反透析法的进一步发展
Pharm Res. 1998 Nov;15(11):1673-9. doi: 10.1023/a:1011992125204.
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Pharmacokinetics and distribution over the blood-brain barrier of zalcitabine (2',3'-dideoxycytidine) and BEA005 (2', 3'-dideoxy-3'-hydroxymethylcytidine) in rats, studied by microdialysis.通过微透析研究扎西他滨（2'，3'-双脱氧胞苷）和BEA005（2'，3'-双脱氧-3'-羟甲基胞苷）在大鼠体内的药代动力学及血脑屏障分布情况。
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HIV-1 protease inhibitors are substrates for the MDR1 multidrug transporter.HIV-1蛋白酶抑制剂是MDR1多药转运蛋白的底物。
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The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.药物转运体P-糖蛋白限制了HIV-1蛋白酶抑制剂的口服吸收和进入脑部。
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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.

DOI:10.1128/AAC.46.7.2284-2286.2002
PMID:12069991
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC127290/
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。