Anti-ischaemic and vasospasmolytic effects of a novel Ca2+ channel blocker, SD-3211, in vitro
| Autor: | Tatsuro Shigei, Fumiko Yamazaki, Nobuaki Miyawaki, Hideyasu Yamauchi, Tatsuji Furuta |
|---|---|
| Rok vydání: | 1991 |
| Předmět: |
medicine.medical_specialty
Contraction (grammar) Potassium Channels Physiology Nicardipine Ischemia Coronary Vasospasm Coronary Disease Myocardial Reperfusion In Vitro Techniques Dogs Physiology (medical) Internal medicine medicine Animals Channel blocker Diltiazem 4-Aminopyridine Pharmacology biology business.industry Arteries medicine.disease Calcium Channel Blockers Coronary Vessels Thiazoles Vasoconstriction Coronary vasospasm Anesthesia Cardiology biology.protein Creatine kinase Rabbits medicine.symptom Amifampridine business medicine.drug |
| Zdroj: | Clinical and experimental pharmacologyphysiology. 18(8) |
| ISSN: | 0305-1870 |
| Popis: | 1. The present study was undertaken to determine the vasospasmolytic activity of a novel non-dihydropyridine type of Ca2+ channel blocker, SD-3211, in isolated canine coronary arteries and its ability to reduce myocardial ischaemic damage in isolated perfused rabbit hearts. 2. The vasospasmolytic effect of SD-3211 was investigated using 3,4-diaminopyridine-induced rhythmic contraction, in comparison with its enantiomer (SD-3212), nicardipine and diltiazem. SD-3211 was shown to reduce the peak tension and increase the contraction frequency. The order of potency for the relaxation of the peak tension was as follows: nicardipine greater than SD-3211 greater than diltiazem greater than SD-3212 and being compatible with that for the relaxant effects of these compounds on KCl-induced contraction in the same specimen. 3. Furthermore, the effect of SD-3211 on myocardial damage due to global ischaemia for 60 min followed by 60 min of reperfusion was examined. SD-3211 at a concentration of 2 X 10(-8) mol/L was given for 40 min before and again for 60 min after the ischaemia. SD-3211 attenuated the increase in leakage of creatine phosphokinase from the hearts and the decrease in pH of perfusate during reperfusion, while concomitantly providing a significant improvement in the post-ischaemic recovery of developed tension. 4. These results suggest that SD-3211 has properties to reduce coronary vasospasm and to provide protection against ischaemic damage, both of which may have beneficial actions in the treatment of ischaemic heart disease. |
| Databáze: | OpenAIRE |
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