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Current Drug Targets

Editor-in-Chief

ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

Review Article

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

Author(s): Marisa Jadna Silva Frederico, Allisson Jhonatan Gomes Castro, Danusa Menegaz, Cahue De Bernardis Murat, Camila Pires Mendes, Alessandra Mascarello, Ricardo Jose Nunes and Fatima Regina Mena Barreto Silva

Volume 18 , Issue 6 , 2017

Page: [641 - 650] Pages: 10

DOI: 10.2174/1389450117666160615084752

Price: $65

Abstract

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.

Keywords: Acyl-hydrazones, glibenclamide derivatives, glucose homeostasis, insulin, pancreatic β-cell, sulfonamides, sulfonylthioureas, sulfonylureas.

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