pone.0202706.g002.tif (358.49 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 2
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posted on 2018-08-16, 17:57 authored by Martina Ceckova, Josef Reznicek, Birgit Deutsch, Martin F. Fromm, Frantisek StaudEffect of efavirenz (10 μM) on transcellular transport of 2 nM[3H]-MPP+ (A) and 10 nM [3H]-lamivudine (C) from the basal to the apical compartment, and intracellular accumulation of [3H]-MPP+ (B) and [3H]-lamivudine (D) in monolayers of MDCK-OCT1, MDCK-OCT2, MDCK-MATE1, MDCK-OCT1-MATE1, MDCK-OCT2-MATE1, and control MDCK-Co cells over 2 hours. Data are shown as means ± SD of at least three independent experiments performed in duplicate. Results were analysed using the multiple t-test **P≤ 0.01 ***P ≤ 0.001.
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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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