The effect of a sulfonylurea, glibenclamide, on the release of insulin, glucagon, and somatostatin was studied in the isolated perfused rat pancreas. At glucose concentrations of 1.1 mM or less, the drug stimulated somatostatin release, whereas glucagon release, after 2-3 min of increase, was markedly inhibited. Insulin release was moderately stimulated, and maximal release occurred relatively ...

Glibenclamide has beneficial effects in animal models of cerebral ischemia. The cellular targets of glibenclamide are proposed to be neurons, endothelial cells, oligodendrocytes and astrocytes. However, independent studies have shown that the SUR1-formed ATP-dependent potassium (KATP) channels are expressed by microglia, which reinforces the idea that glibenclamide may also target microglia and...

background and objective: several studies have found that diazepam decreases serum glucose. meanwhile, glibenclamide is commonly used in diabetes treatment. the objective of this study was to survey the treatment impact of diazepam and glibenclamide on blood glucose and serum lipids in mice with type ii diabetes. materials and methods: in this study, 32 male rats were divided into four groups, ...

Sulfonylureas are anti-diabetic medications that act by inhibiting pancreatic KATP channels composed of SUR1 and Kir6.2. The mechanism by which these drugs interact with and inhibit the channel has been extensively investigated, yet it remains unclear where the drug binding pocket resides. Here, we present a cryo-EM structure of a hamster SUR1/rat Kir6.2 channel bound to a high-affinity sulfony...

Myocardial ATP-sensitive potassium (K(ATP)) channels have been implicated in attenuating cardiac hypertrophy by modulating endothelin-1 concentrations. Sulfonylureas differ in their affinity for cardiac K(ATP) channels and therefore may vary in their effects on left ventricular (LV) mass. We sought to determine the differential effects of sulfonylureas on LV mass in type 2 diabetic patients. Al...

Glibenclamide is an oral hypoglycemic drug commonly prescribed for the treatment of type 2 diabetes mellitus, whose anti-tumor activity has been recently described in several human cancer cells. The mutagenic potential of such an antidiabetic drug and its recombinogenic activity in eukaryotic cells were evaluated, the latter for the first time. The mutagenic potential of glibenclamide in therap...

The objective of this study was to compare effects of RX-871024, a compound with imidazoline structure, and the sulfonylurea glibenclamide, representatives of two groups of ATP-dependent potassium channel (KATP) blockers, on insulin secretion and cytoplasmic free calcium concentration ([Ca2+]i). Furthermore, we studied the interaction of the compounds on these two parameters. The experiments we...

1 It was the aim of our study to investigate the effects of the sulphonylurea glibenclamide on voltage dependent potassium currents in human atrial myocytes. 2 The drug blocked a fraction of the quasi steady state current (ramp response) which was activated positive to -20 mV, was sensitive to 4-aminopyridine (500 microM) and was different from the ATP dependent potassium current IK(ATP). 3 Gli...

BACKGROUND/AIMS Non-alcoholic fatty liver disease (NAFLD), the major hepatic manifestation of type 2 diabetes mellitus, is the most common liver disease in the US. Thiazolidinediones, a commonly used drug class for the treatment of type 2 diabetes, have emerged as a potentially useful treatment for NAFLD. There are, however, lingering concerns about their potential toxicity as well as emerging ...

OBJECTIVE Diabetes mellitus is a syndrome of multiple etiologies. Both type 1 and type 2 diabetes lead to multiple abnormalities of lipid and lipoprotein metabolism. The aim of this investigation was to study the influence of fenofibrate on the blood glucose lowering effect of glibenclamide. MATERIALS AND METHODS Glibenclamide (0.45, 0.23 mg/kg) and fenofibrate (18.1, 9.38 mg/kg) was treated ...