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Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.

作者信息

Vishnuvardhan Daesety, Moltke Lisa L, Richert Clemens, Greenblatt David J

机构信息

Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA.

出版信息

AIDS. 2003 May 2;17(7):1092-4. doi: 10.1097/01.aids.0000060380.78202.b5.

DOI:10.1097/01.aids.0000060380.78202.b5
PMID:12700464
Abstract

The effect of lopinavir on P-glycoprotein-mediated rhodamine 123 efflux was studied in Caco-2 monolayer cells. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers (IC50 1.7 microM). Chronic lopinavir exposure (72 h) in LS 180V cells reduced the content of intracellular Rh123 by approximately 50%, indicating increased efflux activity. In LS 180V cells, lopinavir induced P-glycoprotein immunoreactive protein (up to threefold) and messenger RNA levels in a concentration-dependent fashion.

摘要

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