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

E. Scheufler, C. Heers, B. Wilffert, Thies Peters, G.N. Pierce

Research output: Contribution to journalArticleAcademicpeer-review


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 languageEnglish
Pages (from-to)1145-1147
Number of pages3
JournalArzneimittel-Forschung-Drug research
Issue number11
Publication statusPublished - 22-Oct-1993


  • 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

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