Search results for "Sulfonylurea"
showing 6 items of 26 documents
Molecular Classification of Pesticides Including Persistent Organic Pollutants, Phenylurea and Sulphonylurea Herbicides
2014
Pesticide residues in wine were analyzed by liquid chromatography–tandem mass spectrometry. Retentions are modelled by structure–property relationships. Bioplastic evolution is an evolutionary perspective conjugating effect of acquired characters and evolutionary indeterminacy–morphological determination–natural selection principles; its application to design co-ordination index barely improves correlations. Fractal dimensions and partition coefficient differentiate pesticides. Classification algorithms are based on information entropy and its production. Pesticides allow a structural classification by nonplanarity, and number of O, S, N and Cl atoms and cycles; different behaviours depend …
Circular dichroism studies on the interaction of sulfonylureas with insulin
1976
The interaction of 5 sulfonylurea derivatives with insuline was investigated by means of circular dichroism measurements. It was found that all sulfonylureas investigated decrease the ellipticity band of insulin at 208 nm, whereas the band at 222 nm remains unaffected. It is suggested that these observations are due to a change of the insulin conformation, provoked by the interaction of the drugs with insulin. It is assumed that such an effect on the insulin conformation can influence the binding properties of insulin, e.g. in respect to the insulin aggregation, to the binding to insulin antibodies and to a bound, inactive form of insulin in the plasma. Some other drugs have similar, but mo…
Effect of tormentic acid on insulin secretion in isolated rat islets of langerhans
1989
Tonnentic acid was isolated as the hypoglycemic agent of Poterium ancistroides Desf. The present study reports effects of this compound on isolated islets of Langerhans. We demonstrate that tormentic acid in the presence of 1.66 mM glucose initiates insulin secretion by isolated rat islets of Langerhans in a dose-dependent fashion at concentrations ranging from 0.05 to 0.5 mM. However, the compound has no effect on the insulin-releasing capacity of 16.6 mM glucose. Similar results were obtained with the sulfonylurea glibenclamide (0.01 mM) used as a reference. These results suggest that the hypoglycemic effect of tormentic acid is due to a diect effect of the compound in vitro.
Effects of sulphonylureas on spontaneous motility and induced contractions in rat isolated uterus
1986
Abstract To clarify the action of sulphonylureas on calcium, the effect of tolbutamide and ghbenclamide has been investigated on a Ca-dependent process, the contractile activity of uterine smooth muscle. Both sulphonylureas antagonized the contractions evoked by CaCl2 in a non-competitive manner when the uterus was maintained in depolarizing solution and did not affect the spontaneous contractions of rat uterus. The capacity of tolbutamide and ghbenclamide to relax vanadate-induced contraction of rat uterus in Ca-free medium suggests that sulphonylureas may have an intracellular site of action related to cytosolic free Ca levels, or effect a reduction in Ca action.
A Decision Support Tool for Appropriate Glucose-Lowering Therapy in Patients with Type 2 Diabetes
2015
Contains fulltext : 152084.pdf (Publisher’s version ) (Open Access) BACKGROUND: Optimal glucose-lowering therapy in type 2 diabetes mellitus requires a patient-specific approach. Although a good framework, current guidelines are insufficiently detailed to address the different phenotypes and individual needs of patients seen in daily practice. We developed a patient-specific decision support tool based on a systematic analysis of expert opinion. MATERIALS AND METHODS: Based on the American Diabetes Association (ADA)/European Association for the Study of Diabetes (EASD) 2012 position statement, a panel of 12 European experts rated the appropriateness (RAND/UCLA Appropriateness Method) of tre…
Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repagl…
2004
The 11 C-labeled sulfonylurea receptor 1 (SUR1) ligand (S)-2-(( 11 C)methoxy)-4-(3-methyl-1-(2-piperidine-1-yl-phenyl)- butyl-carbamoyl)-benzoic acid (( 11 C)methoxy-repaglinide) was synthesized in an overall radiochemical yield of 35% after 55 min with a radiochemical purity higher than 99%. This compound is considered for the noninvasive investigation of the SUR1 receptor status of pancreatic b-cells by positron emission tomography (PET) in the context of type 1 and type 2 diabetes. The specific activity was 40-70 GBq/lmol. In vitro testing of the nonradioactive methoxy-repaglinide was performed to characterize the affinity for binding to the human SUR1 isoform. Methoxy-repaglinide induce…