Ammon H P, Melien M C, Pfäffle T
Naunyn Schmiedebergs Arch Pharmacol. 1984 Sep;327(3):234-7. doi: 10.1007/BF00502455.
The effect of thiourea and its derivatives, including methyl- and propylthiouracil as well as the imidazole derivative thiamazole on glucose-induced insulin secretion from incubated rat pancreatic islets was studied. Additionally, the effect of a single oral dose of propylthiouracil on plasma insulin and glucose tolerance was tested in anaesthetized rats. In the presence of 2.8 mM glucose, neither thiourea nor methylthiouracil, propylthiouracil or thiamazole stimulated the secretion of insulin from pancreatic islets. However, in the presence of 11.1 mM glucose all of the above compounds augmented the insulin-releasing properties of glucose in a concentration-related manner-propylthiouracil being the most potent drug. Propylthiouracil (100 and 200 mg/kg body weight) significantly augmented insulin secretion in vivo in response to i.v. glucose (0.5 g/kg). Accordingly, the rate constant of glucose elimination (K-value) was increased. The data suggest that thiourea-containing chemical compounds sensitize pancreatic islets to the insulin-triggering action of glucose.
研究了硫脲及其衍生物（包括甲基硫氧嘧啶和丙基硫氧嘧啶）以及咪唑衍生物甲巯咪唑对孵育的大鼠胰岛葡萄糖诱导的胰岛素分泌的影响。此外，还在麻醉大鼠中测试了单次口服丙基硫氧嘧啶对血浆胰岛素和葡萄糖耐量的影响。在2.8 mM葡萄糖存在的情况下，硫脲、甲基硫氧嘧啶、丙基硫氧嘧啶或甲巯咪唑均未刺激胰岛分泌胰岛素。然而，在11.1 mM葡萄糖存在的情况下，上述所有化合物均以浓度相关的方式增强了葡萄糖的胰岛素释放特性——丙基硫氧嘧啶是最有效的药物。丙基硫氧嘧啶（100和200 mg/kg体重）在体内显著增强了对静脉注射葡萄糖（0.5 g/kg）的胰岛素分泌。因此，葡萄糖消除速率常数（K值）增加。数据表明，含硫脲的化合物使胰岛对葡萄糖的胰岛素触发作用敏感。
