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ANTI‐ISCHAEMIC AND VASOSPASMOLYTIC EFFECTS OF A NOVEL Ca2+ CHANNEL BLOCKER, SD‐3211, IN VITRO
Author(s) -
Miyawaki Nobuaki,
Furuta Tatsuji,
Shigei Tatsuro,
Yamazaki Fumiko,
Yamauchi Hideyasu
Publication year - 1991
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.1991.tb01494.x
Subject(s) - nicardipine , diltiazem , medicine , contraction (grammar) , calcium channel blocker , channel blocker , ischemia , nifedipine , cardiology , anesthesia , pharmacology , calcium
SUMMARY 1. The present study was undertaken to determine the vasospasmolytic activity of a novel non‐dihydropyridine type of Ca 2+ 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 > SD‐3211 > diltiazem > 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 × 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.