pone.0202706.g004.tif (236.92 kB)
Efavirenz reduces renal excretion of lamivudine in rats by inhibiting organic cation transporters (OCT, Oct) and multidrug and toxin extrusion proteins (MATE, Mate) - Fig 4
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posted on 2018-08-16, 17:57 authored by Martina Ceckova, Josef Reznicek, Birgit Deutsch, Martin F. Fromm, Frantisek StaudTotal recovery of [3H]-lamivudine from urine (A) and bile (C), and its accumulation in renal (B) and liver (D) tissue at 240 minutes after i.v. administration with or without co-administration of efavirenz (2.53 mg/kg) or cimetidine (a control inhibitor of the OCT and MATE transporters; 60,6 mg/kg). Data are shown as means ± SD (n = 5) and were analysed using one-way ANOVA followed by Dunnett`s multiple comparison test * P ≤ 0.05, *** P ≤ 0.001, n.s. not significant.
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tissue distributionMDCK-MDR 1OctABCBtranscriptase inhibitortranscellular transportMATE 2-Kvivo pharmacokinetic interaction studyHEK-MATE 2-K cellslamivudine retentionNRTIEFVMRP 2body clearancecation transportersefavirenzABCGtransport assaysfirst-line combination antiretroviral therapyABCCMATE 1-expressing MDCK monolayersAUCHoechst 33342 accumulationtranscriptase inhibitorsSLC 47A P-gpco-administered substratesWistar ratsMDCK-BCRP cellsOCT uptake solute carriersEfavirenzdrug-drug interactionsSLC 22AMDCK-MRP 2 cellsMATE 1-expressing MDCK cellstoxin extrusion proteins
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