Bővebb ismertető
The major steps in the discovery of calcium entry blockers
A. G. Herman
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Summary
The discovery of calcium entry bioclters stresses the importance of the ubiquitous calcium gradient in all living cells.
The chemical structure as well as the functional selectivity of different calcium entry blockers may differ markedly. Some are primarily active on the myocardium, others on erythrocytes or on mast cells. The potent antivasoconstrictor effect of some diphenylmethylderivatives was ascribed to entry blockade as early as 1968. The myocardial effects of verapamil and methoxyverapamil were also attributed to calcium entry blockade. The various mechanisms by which drugs can interfere with Ca^* fluxes through the cell membrane are currently becoming more and more apparent There is no doubt that pharmacologists are getting a better insight into the basic mechanisms of cellular calcium homeostasis and that clinicians are obtaining new valuable medicines.