新型格列本脲衍生物对钾和钙通道胰岛素分泌的作用机制

Title:Mechanism of Action of Novel Glibenclamide Derivatives on Potassium and Calcium Channels for Insulin Secretion

Volume: 18 Issue: 6

关键词: 酰基腙，格列本脲衍生物，葡萄糖体内平衡，胰岛素，胰腺β-细胞，磺酰胺，磺酰硫脲，磺酰脲类。

摘要: Glibenclamide is widely used and remains a cornerstone and an effective antihyperglycemic drug. After the casual discovery of its hypoglycemic potential, this compound was introduced for diabetes treatment. However, the long-term side effects reveal that glibenclamide should be replaced by new molecules able to maintain the health of β-cells, protecting them from hyperstimulation/hyperexcitability, hyperinsulinemia, functional failure and cell death. The aim of this review was to highlight the main mechanism of action of glibenclamide and the influence of its derivatives, such as acylhydrazones, sulfonamides and sulfonylthioureas on β-cells potassium and calcium channels for insulin secretion as well as the contribution of these new compounds to restore glucose homeostasis. Furthermore, the role of glibenclamide-based novel structures that promise less excitability of β-cell in a long-term treatment with effectiveness and safety for diabetes therapy was discussed.

Cite this article as:

Mechanism of Action of Novel Glibenclamide Derivatives on Potassium and Calcium Channels for Insulin Secretion, Current Drug Targets 2017; 18 (6) . https://dx.doi.org/10.2174/1389450117666160615084752