Transport of Angiotensin-Converting Enzyme Inhibitors by H+/Peptide Transporters Revisited

摘要: Angiotensin-converting enzyme (ACE) inhibitors are often regarded as substrates for the H+/peptide transporters (PEPT)1 and PEPT2. Even though conclusions drawn from published data quite inconsistent, in most review articles PEPT1 is claimed to mediate intestinal absorption of ACE thus determine their oral availability. We systematically investigated interaction a series with First, we studied effect 14 including new drugs on uptake dipeptide [14C]glycylsarcosine into human Caco-2 cells constitutively expressing rat renal SKPT In second approach, heterologously expressed PEPT2 was determined. both assay systems, zofenopril fosinopril were found have very high affinity binding peptide transporters. Medium low transporter benazepril, quinapril, trandolapril, spirapril, cilazapril, ramipril, moexipril, quinaprilat, perindopril. For enalapril, lisinopril, captopril, weak or lack found. Transport currents Xenopus laevis oocytes recorded by two-electrode voltage-clamp technique. Statistically significant, but only observed benazepril at spirapril other inhibitors, electrogenic transport activity extremely not measurable all. The present results suggest that do control reabsorption inhibitors.