240 words Introduction: 559 words Discussion: 953 words Abbreviations: SLC, solute carrier; CNT, concentrative nucleoside transporter; ASBT, apical sodium-dependent bile acid transporter; SERT, serotonin transporter; PEPT, peptide transporter; OCTN, organic zwitterion/cation transporter; OATP, organic anion transporting polypeptide; ENT, equilibrative nucleoside transporter; IBD, inflammatory b...

246 words Introduction: 651 words Discussion: 1498 words Abbreviations: PMAT, plasma membrane monoamine transporter; SLC, solute carrier family; OCT, organic cation transporter; ENT, equilibrative nucleoside transporter; MPP, 1-methyl-4phenylpyridinium; DAT, dopamine transporter; SERT, serotonin transporter; CNS, central nervous system; MPTP, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine; TEA, t...

Linagliptin is a highly potent dipeptidyl peptidase-4 (DPP-4) inhibitor approved for the treatment of type 2 diabetes. Unlike other DPP-4 inhibitors, linagliptin is cleared primarily via the bile and gut. We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagliptin disposition in vivo and to assess the po...

Linagliptin is a highly potent dipeptidyl peptidase-4 (DPP-4) inhibitor approved for the treatment of type 2 diabetes. Unlike other DPP-4 inhibitors, linagliptin is cleared primarily via the bile and gut. We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagliptin disposition in vivo and to assess the po...

Many endogenous compounds and xenobiotics are organic cations that rely on polyspecific organic cation transporters (OCTs) to traverse cell membranes. We recently cloned a novel human plasma membrane monoamine transporter (PMAT) that belongs to the equillibrative nucleoside transporter (ENT) family. We have reported previously that, unlike other ENTs, PMAT (also known as ENT4) is a Na+-independ...

This study examined the effect of estrogen (17beta-estradiol) on renal handling of organic cation, tetraethylammonium (TEA), both in vivo and in vitro. Clearance of TEA in ovariectomized (OVX) mice was increased by 38% above intact animals, which was able to be returned to control level by estrogen supplementation. The mechanism of this effect was examined in isolated mouse renal proximal tubul...

Patients with chronic hepatitis C viral infection underwent liver biopsies and laboratory studies for evaluation and to determine subsequent treatment. Changes in status of drug metabolism and disposition may vary with chronic hepatitis C stage and should be assessed. Total RNA was extracted from liver biopsy specimens (n = 63) and reverse transcribed to yield cDNA. Relative mRNA levels of drug...