Interference of N-(1-[4-(4-fluophenoxy)butyl]-piperidinyl)-N-methyl-2-benzothiazolamin e with Na+/H+exchange and Na+/Ca2+exchange in purified cardiac sarcolemmal membranes
| Autor: | Scheufler, E., Heers, C., Wilffert, B., Peters, Thies, Pierce, G.N. |
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| Přispěvatelé: | Methods in Medicines evaluation & Outcomes research (M2O), Reproductive Origins of Adult Health and Disease (ROAHD) |
| Jazyk: | angličtina |
| Rok vydání: | 1993 |
| Předmět: |
nonhuman
heart muscle fiber membrane article sodium ion ion exchange CAS 104606-13-5 R 56865 animal tissue N-[1-[4-(4-fluorophenoxy)butyl]-piperidinyl]-N-methyl-2-be nzothiazolamine priority journal cattle concentration response dog calcium ion controlled study pharmacology dichlorobenzamil n [1 [4 (4 fluorophenoxy)butyl] 4 piperidinyl] n methyl 2 benzothiazolamine proton |
| Zdroj: | Arzneimittel-Forschung-Drug research, 43(11), 1145-1147 |
| ISSN: | 0004-4172 |
| Popis: | The effect of R 56865 (N-[1-[4-(4-fluorophenoxy) butyl]-piperidinyl]-N-methyl-2-benzothiazolamine, CAS 104606-13-5) on Na+/H+exchange and Na+/Ca2+exchange was studied in isolated cardiac sarcolemmal vesicles. R 56865 inhibited Na+/H+exchange with an ED50of 180 μmol/l at a concentration of 0.05 mmol/l Na+. The potency of R 56865 decreased with increasing concentrations of Na+. Na+/Ca2+exchange was also inhibited. The ED50amounted to 45 μmol/l. This ED50was close to that of the reference compound dichlorobenzamil (ED50= 27 μmol/l). The inhibitory potency of R 56865 on Na+/H+and Na+/Ca2+exchange is far too low to explain the already reported beneficial effects of this inhibitor of Na+and Ca+overload during ouabain intoxication and ischemia and reperfusion. |
| Databáze: | OpenAIRE |
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