Grund V R, Martino R, Hunninghake D B
Clin Pharmacol Ther. 1980 Sep;28(3):392-7. doi: 10.1038/clpt.1980.178.
The effects of an H2-histamine receptor antagonist, cimetidine, on histamine-induced changes in plasma levels of insulin, free fatty acids (FFAs), and glucose was examined in a randomized, double-blind study in six fasted men. The intravenous infusion of histamine at an average rate of 0.13 microgram/kg/min for 20 min caused a rapid rise in plasma insulin levels throughout the infusion period (p < 0.05). Insulin levels rose 23% above baseline after 5 min of infusion and continued to 51% above baseline 10 min after the infusion ended. Cimetidine pretreatment (300 mg intravenously) inhibited histamine-induced insulin secretion by 98% or more at each point during the infusion (p < 0.05), but did not inhibit an effect of histamine to elevate plasma FFA levels. Plasma FFA levels were increased 33% by histamine alone and 41% by histamine when subjects had been pretreated with cimetidine (p < 0.05). Plasma glucose levels were not affected by histamine or cimetidine. These findings demonstrate that histamine is capable of inducing insulin secretion in man at low doses. Blockade of this effect with cimedine suggests that the mechanism of histamine-induced insulin secretion involves the H2-histamine receptor.
在一项针对六名禁食男性的随机双盲研究中，检测了H2组胺受体拮抗剂西咪替丁对组胺诱导的胰岛素、游离脂肪酸（FFA）和葡萄糖血浆水平变化的影响。以平均0.13微克/千克/分钟的速率静脉输注组胺20分钟，在整个输注期间导致血浆胰岛素水平迅速升高（p<0.05）。输注5分钟后，胰岛素水平比基线升高23%，输注结束后10分钟继续比基线升高51%。西咪替丁预处理（静脉注射300毫克）在输注期间的每个时间点均抑制组胺诱导的胰岛素分泌达98%或更多（p<0.05），但不抑制组胺升高血浆FFA水平的作用。单独使用组胺时血浆FFA水平升高33%，在受试者用西咪替丁预处理后组胺使血浆FFA水平升高41%（p<0.05）。血浆葡萄糖水平不受组胺或西咪替丁的影响。这些发现表明，组胺能够在低剂量时诱导人体胰岛素分泌。用西咪替丁阻断这种作用表明，组胺诱导胰岛素分泌的机制涉及H2组胺受体。
