ABSTRACT. Renal excretion of organic anions and cations is mediated by the ion transporter family (SLC22A). In this study, mRNA levels transporters were quantified real-time PCR in normal parts renal tissues from seven nephrectomized patients with cell carcinoma, distributions localization human (h)OAT1, hOAT3, hOCT2 proteins investigated immunohistochemical analyses kidney. The expression level hOAT3 was highest among family, followed that hOAT1 mRNA. OCT hOCTN2 higher than hOCTN1. hOCT1...

A complementary DNA (cDNA) encoding the rat H+/peptide cotransporter (PepT1) was isolated, and transport characteristics of orally active beta-lactam antibiotics were assessed by measuring uptake into Xenopus oocytes expressing PepT1. The PepT1 cDNA encoded a 710-amino acid protein with 77% identity to rabbit message for approximately 2.9 kilobases found predominantly in small intestine, whereas reverse transcription-polymerase chain reaction amplification revealed that expressed both...

We have isolated a kidney-specific organic cation transporter, rat OCT2, which is distinct from OCT1 (Okuda M, Saito H, Urakami Y, Takano M and Inui K (1996) Biochem Biophys Res Commun 224:500-507). In our study, the functional characteristics membrane localization of OCT2 were investigated by uptake studies using MDCK cells transfected with or cDNA (MDCK-OCT1 MDCK-OCT2) immunological studies. Tetraethylammonium (TEA) both MDCK-OCT1 MDCK-OCT2 was markedly elevated when TEA added to...

We have cloned a cDNA coding for novel member of organic anion transporter, designated OAT-K1, expressed specifically in the kidney rats. The rat OAT-K1 (2788 base pairs) had an open reading frame encoding 669-amino acid protein (calculated molecular mass 74 kDa) which shows 72% identity with liver oatp. Northern hybridization and reverse transcription-coupled polymerase chain reaction revealed that messenger RNA transcript is predominantly kidney. By use stable LLC-PK1 cell monolayers...

The bioavailability of structurally unrelated drugs is limited by active secretion via the multidrug resistance gene (MDR1) product P-glycoprotein (Pgp) from enterocyte into lumen as well intestinal metabolism cytochrome P450 IIIA4 (CYP3A4). In present study, we analyzed whether genetic polymorphism MDR1 had some influence on expression levels Pgp and CYP3A4 tacrolimus concentration/dose ratio over first postoperative days in recipients living-donor liver transplantation (LDLT). Genotyping...

The organic cation transporter (OCT) mediates translocation of various cationic molecules including drugs, toxins and endogenous substances. We examined gender differences in the expression rat (r) OCT2 kidney. Slices basolateral membrane vesicles male kidney showed a higher transport activity for tetraethylammonium than those female levels rOCT2 mRNA protein males were much females. There was no difference rOCT1 rOCT3. These findings suggest that is responsible renal activity.

The interaction of imatinib mesilate with P-glycoprotein (P-gp) was examined using pig kidney epithelial LLC-PK1 cells versus L-MDR1 cells, which overexpress human P-gp on the apical membrane. basal-to-apical transport in significantly exceeded that parental LLCPK1 cells. intracellular accumulation after its basal application to and 35% 15%, respectively. A modulator, cyclosporin A, inhibited also increased by A. rhodamine 123 efflux assay showed K562/DXR P-gp, could be blocked markedly a...

The accumulation and the transepithelial transport of p.o. cephalosporins by monolayers human intestinal epithelial cell line Caco-2 grown on microporous membrane filters were evaluated. Cephradine was accumulated concentratively in from apical side, transported to basolateral side. apical-to-basolateral cephradine temperature-dependent sensitive pH with optimal 6.0 6.5. efflux side also more rapid than its cephradine, cephalexin cefixime, all agents, significantly higher those cefotiam, a...

Rat (r) OCT2 was identified as the second member of organic cation transporter (OCT) family, and is predominantly expressed in kidney. We reported previously that rOCT2 responsible for gender differences renal basolateral membrane transport activity. As expression males much higher than females, we hypothesized may be under control sex hormones. Treatment male female rats with testosterone significantly increased levels mRNA protein kidney, whereas estradiol treatment moderately decreased...

Newly synthesized rifamycin derivatives, KRM-1648, KRM-1657, KRM-1668, KRM-1686, and KRM-1687, having the chemical structures of 3'-hydroxy-5'-(4-alkylpiperazinyl)-benzoxazinorifamycins (alkyl residues: isobutyl, propyl, sec-butyl, sec-butyl [R configuration], [S respectively), were studied for their in vitro antimycobacterial activities. Representative (KRM-1648) MICs 90% strains tested, determined by agar dilution method on 7H11 medium, various pathogenic mycobacteria (9 species, 174...

The purpose of this study was to explore the role organic anion-transporting polypeptide (OATP) 1A2, which is encoded by SLCO1A2, in cellular uptake Bcr-Abl tyrosine kinase inhibitor imatinib, and relationship between SLCO1A2 polymorphisms pharmacokinetics imatinib patients with chronic myeloid leukemia (CML). Imatinib significantly enhanced OATP1A2-transfected human embryonic kidney (HEK) 293 cells (P = 0.002). Naringin, an OATP1A2 inhibitor, decreased transport HEK293 cells, intestinal...

High mortality of acute kidney injury (AKI) is associated with lung (ALI), which a typical complication AKI. Although it suggested that dysregulation salt and water channels following AKI plays pivotal role in ALI, the mechanism its has not been elucidated. Here, we examined involvement oxidative stress-inducing uremic toxin, indoxyl sulfate (IS), pulmonary predominant channel, aquaporin 5 (AQP-5), bilateral nephrectomy (BNx)-induced model rats. BNx evoked increases serum creatinine (SCr),...

We have isolated a cDNA coding new organic anion transporter, OAT-K2, expressed specifically in rat kidney. The OAT-K2 had an open reading frame encoding 498-amino acid protein (calculated molecular mass of 55 kDa) that shows 91% identity with the kidney-specific OAT-K1. Reverse transcription-coupled polymerase chain reaction analyses revealed mRNA was predominantly proximal convoluted tubules, straight and cortical collecting ducts. When Xenopus oocytes, stimulated uptake hydrophobic...

Living-donor liver transplantation (LDLT) and subsequent immunosuppressive therapy with tacrolimus have been cornerstones in the recovery of patients from end-stage failure, but there has no critical dosage regimen for therapy, especially initial dosage. In this study, we examined whether absorptive barriers, multidrug resistance protein (MDR1), or cytochrome P450 IIIA4 (CYP3A4) are important pharmacokinetic factors prognostic indicators LDLT outcome.We used competitive polymerase chain...

The localization and transport characteristics of dipeptide transporters the intestinal epithelial cell line Caco-2 were examined by measuring intracellular accumulation transcellular flux Bestatin, a dipeptide-like anticancer agent. When added to apical surface monolayers grown on microporous membrane filters, Bestatin was accumulated in cells transported unidirectionally basolateral side. cellular uptake from as well inhibited excess dipeptides. dependent pH incubation medium with an...