Effects of piperazine derivatives on the activity of frog skeletal muscle fibers
| Autor: | Vydevska M, Mileva K, Radicheva N |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Pharmacology
medicine.medical_specialty Dose-Response Relationship Drug Chemistry Antinematodal Agents Cell Membrane Action Potentials Rana esculenta Piperazines Rana Electrophysiology Piperazine chemistry.chemical_compound Gastrocnemius muscle Membrane Endocrinology Internal medicine Extracellular medicine Biophysics Membrane channel GRENOUILLE Animals Muscle Skeletal |
| Zdroj: | General pharmacology. 26(6) |
| ISSN: | 0306-3623 |
| Popis: | 1. This study was undertaken to characterize the effects of some piperazine derivatives on excitable cell membranes. Three original Bulgarian compounds with favorable effects on cardiovascular and nervous system--piperazine derivatives with code names P-11 (N1-[3-oxo-3-phenyl-2-methyl-propyl]-N4-[trans-3-hydroxy-1,2,3,4- tetrahydro-2-naphthyl]-piperazine dihydrochloride), AS2 (N1-benzhydryl-N4-allyl piperazine dihydrochloride) and 35-M (Schiff's base of N1-benzhydryl-N4-aminopiperazine with triacetonamine, dioxalate salt) were tested in experiments with conventional microelectrode technique on isolated frog muscle fibers. 2. After 30-min treatment with tested drugs at concentrations of 10-100 microM the recorded intra-(ICAP) and extracellular action potentials (ECAPs) showed an amplitude decrease and duration increase. The total ionic current (Ii) decreased as the outward phase was almost abolished by P-11. The propagation velocity (PV) of excitation and the twitch amplitude also decreased. These changes were agent- and concentration-dependent. 3. The effect potency of the agents diminished in the following order: P-11 > AS2 > 35-M. 4. Concentrations higher than 100 microM for all agents completely, but reversibly, inhibited membrane excitability. 5. The results demonstrate compound- and concentration-induced modulation of Ca2+ current with blockade of Ca(2+)-dependent K+ and Cl- membrane channels of muscle fiber treated with the compound tested. |
| Databáze: | OpenAIRE |
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