De Marinis L, Merlini G, Makhoul O, Barbarino A
J Endocrinol Invest. 1982 Mar-Apr;5(2):121-4. doi: 10.1007/BF03350503.
Extensive in vitro studies have demonstrated that an increase in the concentration of Ca2+ in the cytosol of the beta-cell of islets of Langherhans is essential for the glucose-stimulated insulin release. However, there are controversies as to whether both phases of insulin release are equally dependent upon glucose-stimulated uptake of extracellular calcium. Previous studies performed in vivo, have demonstrated an inhibitory effect of verapamil, an organic antagonist of calcium transport into cells, on the release of insulin induced by an oral glucose load. The present study was designed to investigate whether calcium antagonists are capable of inhibiting the rapid release of insulin that follows the iv infusion of glucose. Verapamil, infused into normal subjects for different periods of time before the iv administration of glucose was ineffective in inhibiting the rapid release of insulin, even when it was infused for 1 h before the glucose stimulus was applied. The present results obtained in vivo confirm some previous in vitro data showing that the first phase insulin release is not inhibited by calcium antagonist, agents known to block the uptake of calcium from extracellular sources.
大量的体外研究表明,胰岛β细胞胞质溶胶中Ca2+浓度的增加对于葡萄糖刺激的胰岛素释放至关重要。然而,关于胰岛素释放的两个阶段是否同样依赖于葡萄糖刺激的细胞外钙摄取存在争议。先前在体内进行的研究表明,维拉帕米(一种细胞钙转运的有机拮抗剂)对口服葡萄糖负荷诱导的胰岛素释放具有抑制作用。本研究旨在调查钙拮抗剂是否能够抑制静脉注射葡萄糖后胰岛素的快速释放。在静脉注射葡萄糖前不同时间段向正常受试者输注维拉帕米,即使在葡萄糖刺激前输注1小时,也无法有效抑制胰岛素的快速释放。目前在体内获得的结果证实了一些先前的体外数据,表明第一阶段胰岛素释放不受钙拮抗剂的抑制,钙拮抗剂是已知可阻断从细胞外来源摄取钙的药物。