Influence of coronary dilators on the uptake of serotonin by human platelets and adrenaline by chromaffine granules.
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Chemotaxis by electroporated rabbit peritoneal neutrophils in the absence of Ca2+ is only slightly different from that in the presence of Ca2+. Pretreatment of neutrophils with quin2-AM causes inhibition of chemotaxis. Calcium antagonists as nitrendipine and verapamil are inhibitory in nanomolar concentrations, while 10(5) times higher concentrations are required for inhibition of chemotaxis by neutrophils which were not electroporated. The results support the hypothesis that Ca2+ from Ca(2+)-storing organelles is of importance for chemotaxis, but that chemotaxis is not dependent on changes in cytoplasmic Ca2+ concentrations.
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Felodipine inhibits fMet-Leu-Phe or ionophore A23187-induced exocytosis in rabbit peritoneal polymorphonuclear leukocytes (PMNs), in the concentration range 1-50 microM. Activation of the metabolic burst, and migration of PMNs towards fMet-Leu-Phe are equally inhibited by felodipine in the same concentration range. The effect is not due to blocking of calcium channels in the plasma membrane, because the degree of inhibition remains the same when Ca2+ is omitted from the medium. Felodipine interferes with ionophore A23187-induced association of 45Ca with the PMN but this interference occurs at lower concentrations than the inhibition of exocytosis. Hypotonic hemolysis of erythrocytes is inhibited by felodipine; maximal protection against hemolysis occurs at a concentration of 50 microM felodipine. It is suggested that at least a part of the inhibiting effect on PMN functions might be due to an anesthetic-like membrane effect of felodipine.
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Several new prenylnaphthohydroquinone derivatives have been prepared through the Diels-Alder condensation between alpha-myrcene and 1,2-benzoquinone and evaluated for their cytotoxic activity against A-549, HT-29 and MB-231 cultured cell lines. All of them have shown GI50 values in the microM level.