Elferink J G, Deierkauf M
Department of Medical Biochemistry, University of Leiden, Sylvius Laboratories, The Netherlands.
Biochem Pharmacol. 1988 Feb 1;37(3):503-9. doi: 10.1016/0006-2952(88)90221-3.
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.
非洛地平在1-50微摩尔浓度范围内可抑制家兔腹腔多形核白细胞(PMN)中fMet-Leu-Phe或离子载体A23187诱导的胞吐作用。在相同浓度范围内,非洛地平同样可抑制PMN的代谢爆发激活以及其向fMet-Leu-Phe的迁移。该作用并非由于阻断质膜上的钙通道,因为当培养基中省略Ca2+时,抑制程度保持不变。非洛地平会干扰离子载体A23187诱导的45Ca与PMN的结合,但这种干扰发生的浓度低于对胞吐作用的抑制浓度。非洛地平可抑制红细胞的低渗溶血;在非洛地平浓度为50微摩尔时对溶血的保护作用最大。提示非洛地平对PMN功能的抑制作用至少部分可能归因于其类似麻醉剂的膜效应。