Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 1145-1147 |
| Number of pages | 3 |
| Journal | Arzneimittel-Forschung-Drug research |
| Volume | 43 |
| Issue number | 11 |
| Publication status | Published - 22-Oct-1993 |
Keywords
- CAS 104606-13-5
- N-[1-[4-(4-fluorophenoxy)butyl]-piperidinyl]-N-methyl-2-be nzothiazolamine
- pharmacology
- R 56865
- calcium ion
- dichlorobenzamil
- n [1 [4 (4 fluorophenoxy)butyl] 4 piperidinyl] n methyl 2 benzothiazolamine
- proton
- sodium ion
- animal tissue
- article
- cattle
- concentration response
- controlled study
- dog
- heart muscle fiber membrane
- ion exchange
- nonhuman
- priority journal