Improved Insulin Receptor Assay: Effects of an Antidiabetic Sulphonylurea on Liver Membrane Insulin Receptors From Obese Hyperglycaemic Mice

Greenstein, Ben

doi:10.1111/j.1476-5381.1979.tb13682.x

Cited by 23 publications

(10 citation statements)

References 14 publications

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“…Chlorpropamide is able to inhibit glucose output from the liver in patients with type 2 diabetes (Best, Judzewitsch, Pfeifer, Beard, Halter and Porte 1982); glipizide reduces in rats glucosamineinduced glycogenolysis (Block, Daturi and Tommasini 1980a), and chlorpropamide reduces glucagon-induced glycogenolysis in the perfused rat liver (Blumenthal and Whitmer 1979). On the other hand, evidence has accumulated that long-term treatment with SUs increases the responsiveness of hepatocytes (Greenstein 1979), muscular cells (Feldman and Lebovitz 1969;Bloch, Daturi and Tommasini 1980b) and adipocytes (Maloff and Lockwood 1981) to insulin. Insulin receptors studies were not performed in our trial; further investigations are required to evaluate if the effect of the two SUs is mediated by modifications of the number of insulin receptors (Feinglos and Lebovitz 1978) or by modifications in their binding affinity for insulin (Maloff and Lockwood 1981).…”

Section: Discussionmentioning

confidence: 96%

Sulfonylureas Enhance In Vivo the Effectiveness of Insulin in Type 1 (Insulin Dependent) Diabetes Mellitus

et al. 2008

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Indirect evidence suggests that sulfonylureas, in addition to stimulating insulin release, exert additional effects at extrapancreatic levels which are of value in the management of type 2 diabetes. In order to characterize in vivo some of these effects, insulin sensitivity was studied in 9 type 1 diabetics with no residual insulin secretory activity, during treatment with chlorpropamide (250 mg b.i.d. for 8 days) and with glipizide (5 mg t.i.d. for 8 days). Employing the glucose clamp technique with the aid of an artificial pancreas (Biostator), glucose disposal during insulin infusion (0.1 U/kg in 60 min) was calculated by the amount of glucose required to keep the blood glucose at preinfusion levels. Chlorpropamide and glipizide administration was accompanied by a significant increase of the amount of glucose required to clamp blood glucose levels, while serum (free) insulin levels were superimposable during the different clamping studies. In the absence of endogenous insulin release, these data strongly suggest that the two sulfonylureas employed enhance in vivo the peripheral sensitivity to insulin. Further studies are required to indicate a preferential site of action (liver, muscle, adipose tissue) of sulfonylureas.

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Section: Discussionmentioning

confidence: 96%

Sulfonylureas Enhance In Vivo the Effectiveness of Insulin in Type 1 (Insulin Dependent) Diabetes Mellitus

et al. 2008

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“…Direct effects on the pancreas can be demonstrated in vitro by a concentration of glibenclamide as low as 2 nmol/1 [42]. In addition it is known that sulphonylureas are without effect in totally pancreatectomized animals [43], and in insulin-dependent diabetics [44], but it has been shown that sulphonylureas may increase insulin receptors in target tissues [45,46]. From available evidence it seems likely that the main effect of sulphonylureas in non insulin dependent diabetes, is to increase the sensitivity of the B-cell response to changes in blood glucose concentrations.…”

Section: Discussionmentioning

confidence: 99%

Hormonal and metabolic effects of chlorpropamide, glibenclamide and placebo in a cross-over study in diabetics not controlled by diet alone

et al. 1981

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Summary. Twenty diabetic patients, whose hyperglycaemia had been shown to fail to respond to at least one month's dietary treatment, completed a crossover study in order to: 1) compare the effectiveness of two sulphonylureas, chlorpropamide and glibenclamide, and 2) study the effects of sulphonylureas on insulin secretion and on biochemical indices of glucose intolerance. Fasting blood glucose fell on active treatment from 10.7 _-2 0.6 (mean _.+ SEM) to 6.6 + 0.7 mmol/l and rose again to 10.6 z 0.7 after 4 months placebo. A second period of 4 months sulphony/urea therapy resulted in a comparable fatl in blood glucose (to 6.9 + 0.7 mmol/1) and 'a similar relapse was seen after the second placebo period (to 10.5 ___ 0.9 mmol/i). Glucose tolerance and associated insulin secretion improved markedly on active treatment, with ketone bodies, non-esterified fatty acids, and glycerol falling to within the reference range. Sulphonylurea therapy was associated with a small but significant increase in the fasting insulin level. These effects were nearly all reversed 4 months after withdrawal of the sulphonylureas. No marked changes were found in growth hormone, lactate, pyruvate, lactate/pyruvate ratio or fasting cholesterol, trigtycerides and lipoproteins. On a weight basis, glibenclamide was 26 times more potent than chlorpropamide and, in the doses used in this study, their biochemical effects were indistinguishable. The effects of these two sulphonylureas seem most likely to be mediated by a direct stimulation of insulin secretion by the B-cell.

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“…Metformin directly affects insulin receptor binding in a variety of cell systems [4,5,6,11]. It selectively increases the number of low affinity binding sites [4,5].…”

Section: Introductionmentioning

confidence: 99%

Three different classes of oral antidiabetic drugs do not increase insulin binding and insulin-inducedRNA synthesis in human fibroblast cultures

1985

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We describe insulin binding and insulin-mediated RNA synthesis on seven human fibroblasts strains in culture initiated from skin biopsies in the presence of three oral antidiabetic agents, Metformin, Gliquidone, and a non-sulfonylurea antidiabetic drug (B X DF 591 ZW), which belong to different chemical classes. At least at a nontoxic pharmacologic concentration of 1 microgram/ml these drugs did not influence the number and affinity of insulin receptors, nor did they increase the insulin-mediated RNA synthesis. We conclude that cultured fibroblasts do not represent the proper target for an evaluation of an extrapancreatic action of oral antidiabetic drugs.

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Improved Insulin Receptor Assay: Effects of an Antidiabetic Sulphonylurea on Liver Membrane Insulin Receptors From Obese Hyperglycaemic Mice

Cited by 23 publications

References 14 publications

Sulfonylureas Enhance In Vivo the Effectiveness of Insulin in Type 1 (Insulin Dependent) Diabetes Mellitus

Sulfonylureas Enhance In Vivo the Effectiveness of Insulin in Type 1 (Insulin Dependent) Diabetes Mellitus

Hormonal and metabolic effects of chlorpropamide, glibenclamide and placebo in a cross-over study in diabetics not controlled by diet alone

Three different classes of oral antidiabetic drugs do not increase insulin binding and insulin-inducedRNA synthesis in human fibroblast cultures

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