Results 261 to 270 of about 2,674,072 (303)

Direct photoaffinity labeling of the putative sulfonylurea receptor in rat β-cell tumor membranes by [3H]glibenclamide

open access: yesFEBS Letters, 1988
The oral antidiabetic sulfonylurea [3H]glibenclamide specifically binds to plasma membranes from a rat β-cell tumor indicating a receptor for sulfonylureas in these membranes.
Werner Kramer
exaly   +2 more sources

Sulfonylurea receptors and mechanism of sulfonylurea action

Experimental and Clinical Endocrinology & Diabetes, 2009
Binding of hypoglycemic sulfonylureas and their analogues to the sulfonylurea receptor in the beta-cell plasma membrane mediates closure of the ATP-sensitive K+-channel (KATP-channel) and thereby stimulation of insulin release. The sulfonylurea receptor is a member of the traffic ATPase family with two intracellular nucleotide binding folds.
U, Panten   +2 more
openaire   +2 more sources

Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies [PDF]

open access: yesEuropean Journal of Medicinal Chemistry, 2012
The combination of antagonism at histamine H3 receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated with obesity.
Núria Cirauquí   +2 more
exaly   +1 more source

Characterization and Significance of Sulfonylurea Receptors

Diabetes Care, 1990
This study describes and characterizes a putative sulfonylurea receptor. The radioligand used was [3H]glipizide (9 Ci/mmol). The β-cell plasma membranes were derived from a transplantable rat insulinoma generated by subcutaneous injection of RINm5F cells and purified by ultracentrifugation on a 15–55% sucrose gradient. Specific binding of [3H]glipizide
L, Siconolfi-Baez   +2 more
openaire   +2 more sources

Pancreatic and Extrapancreatic Sulfonylurea Receptors

Hormone and Metabolic Research, 1992
The hypoglycemic effect of sulfonylureas and their analogues results from their binding to a high affinity site in the B-cell plasma membrane. This site seems to be a structural component of the ATP-sensitive K(+)-channel and represents the pancreatic sulfonylurea receptor.
U, Panten   +2 more
openaire   +2 more sources

The Mitochondrial Sulfonylurea Receptor: Identification and Characterization

Biochemical and Biophysical Research Communications, 1997
Biochemical identification of mitochondrial sulfonylurea receptors has been carried out through binding studies performed with [3H]glibenclamide. The presence of a single class of low affinity binding sites for glibenclamide in the inner mitochondrial membrane has been found, with a KD of 360 +/- 48 nM and BMAX of 48 +/- 7 pmoles/mg in beef heart ...
A, Szewczyk   +3 more
openaire   +2 more sources

Expression of sulfonylurea receptors in rat taste buds

Acta Histochemica, 2011
To test the possibility that a fast-onset promoting agent repaglinide may initiate prandial insulin secretion through the mechanism of cephalic-phase insulin release, we explored the expression and distribution character of sulfonylurea receptors in rat taste buds. Twenty male Wistar rats aged 10 weeks old were killed after general anesthesia.
Dian-Xin, Liu   +4 more
openaire   +2 more sources

A New Mesangial Triumvirate: Sulfonylureas, Their Receptors and Endosulfines

Nephron Experimental Nephrology, 2002
Although sulfonylureas have long been therapeutically utilized for their hypoglycemic properties in type 2 diabetic patients, there is a paucity of clinical or experimental data that suggests that this pharmacotherapeutic class confers a benefit on the course of diabetic renal disease.
Jerry, Yee, Balàzs, Szamosfalvi
openaire   +2 more sources

Insulin Secretagogues, Sulfonylurea Receptors and KATP Channels

Current Pharmaceutical Design, 2005
ATP-sensitive K+ channels, termed K(ATP) channels, provide a link between cellular metabolism and membrane electrical activity in a variety of tissues. Channel isoforms have been identified and are targets for compounds that both stimulate and inhibit their activity resulting in membrane hyperpolarization and depolarization, respectively.
J, Bryan   +4 more
openaire   +2 more sources

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