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| Content Provider | Springer Nature Link |
|---|---|
| Author | Kennedy, D. J. Raldua, D. Thwaites, D. T. |
| Copyright Year | 2005 |
| Abstract | Selective pharmacological Na+/H+ exchange (NHE) inhibitors were used to identify functional NHE isoforms in human small intestinal enterocytes (Caco-2) and to distinguish between direct and indirect effects on transport via the intestinal di/tripeptide transporter hPepT1. The relative potencies of these inhibitors to inhibit 22Na+ influx identifies NHE3 and NHE1 as the apical and basolateral NHE isoforms. The Na+-dependent (NHE3-sensitive) component of apical dipeptide ([14C] Gly-Sar) uptake was inhibited by the selective NHE inhibitors with the same order of potency observed for inhibition of apical 22Na+ uptake. However, 5-(N-ethyl-N-isopropyl) amiloride (EIPA) also reduced [14C]Gly-Sar uptake in the absence of Na+ and this inhibition was concentration and pH (maximal at pH 5.5) dependent. NHE3 inhibition by S1611 and S3226 modulates dipeptide uptake indirectly by reducing the transapical driving force (H+ electrochemical gradient). EIPA (at 100 μM) has similar effects, but at higher concentrations (>200 μM) also has direct inhibitory effects on hPepT1. |
| Starting Page | 1621 |
| Ending Page | 1631 |
| Page Count | 11 |
| File Format | |
| ISSN | 1420682X |
| Journal | Cellular and Molecular Life Sciences |
| Volume Number | 62 |
| Issue Number | 14 |
| e-ISSN | 14209071 |
| Language | English |
| Publisher | Birkhäuser-Verlag |
| Publisher Date | 2005-06-17 |
| Publisher Place | Basel |
| Access Restriction | Subscribed |
| Subject Keyword | H+-coupled transport dipeptide transport intestinal absorption PepT1 Na+/H+ exchange NHE3 EIPA amiloride Biomedicine general Life Sciences Biochemistry Cell Biology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cell Biology Molecular Biology Molecular Medicine Pharmacology Cellular and Molecular Neuroscience |
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