Drugs online research references
Br J Pharmacol. 1997 Feb;120(3):476-80.
Pharmacological characterization of the sulphonylurea receptor in rat isolated aorta.
Loffler C, Quast U.
Department of Pharmacology, Medical Faculty, University of Tubingen, Germany.
1. The binding of the sulphonylurea [3H]-glibenclamide, a blocker of adenosine 5'-triphosphate (ATP)-sensitive K+ channels (KATP channels), was studied in endothelium-denuded rings from rat aorta. 2. [3H]-glibenclamide labelled two classes of binding sites with KD values of 20 +/- 5 nM and 32 +/- 1 microM. The high affinity component, which comprised 17% of total binding at 1 nM [3H]-glibenclamide, had an estimated binding capacity of 150 fmol mg-1 wet weight. 3. Other sulphonylureas such as glipizide and glibornuride and the sulphonylurea-related carboxylate, AZ-DF 265, inhibited high affinity [3H]-glibenclamide binding with the potencies expected from their K+ channel activity. At very high concentrations, AZ-DF 265 and glipizide started to interact also with the low affinity component of [3H]-glibenclamide binding. 4. Openers of the ATP-sensitive K+ channel belonging to different structural groups inhibited only the high affinity [3H]-glibenclamide binding; the potencies in this assay were similar to those obtained in functional (i.e. vasorelaxation) studies. 5. High affinity [3H]-glibenclamide binding was abolished by prolonged hypoxia combined with metabolic inhibition. 6. The data indicate that the high affinity component of [3H]-glibenclamide binding mediates the block of the KATP channel by the sulphonylureas in rat aorta; hence, it represents the sulphonylurea receptor in this vessel. The pharmacological properties of this binding site resemble those of the binding site for the openers of the KATP channel; present evidence suggests that these two classes of sites are negatively allosterically coupled.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9031752&dopt=Abstract
J Clin Endocrinol Metab. 1977 Sep;45(3):601-4.
Potentiation of insulin action: a probable mechanism for the anti-diabetic action of sulfonylurea drugs.
Lebovitz HE, Feinglos MN, Bucholtz HK, Lebovitz FL.
Insulin action was assessed by measuring insulin-mediated glucose disposal (KI) in 13 non-ketotic diabetic patients both before treatment and after normalization of plasma glucose by diet (5 patients) or sulfonylurea (glipizide) therapy (8 patients). While the KI of the diet-treated group was unchanged by therapy, that of the glipizide-treated group was significantly increased. The data show that chronic glipizide therapy is associated with a potentiation of insulin action, which may account for the major anti-diabetic effect of this drug.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=903405&dopt=Abstract
Arzneimittelforschung. 1997 Jan;47(1):97-100.
Studies on the phototoxic effects of oral antidiabetics and diuretics.
Selvaag E.
Department of Dermatology, Ullevaal Hospital, University of Oslo, Norway.
A number of sulphonamide derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics (bemetizide, bendroflumethiazide, benzylhydrochlorothaizide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide) were investigated for phototoxicity in a cell culture model. Cell death dependent on UVA fluence and test substance concentration was observed in the presence of the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics bemetizide, bendroflumethiazide, benzylhydroxhlorothiazide, bumetanide, butizide, hydrochlorothiazide, hydroflumethiazide, piretanide, polythiazide and trichlormethiazide. Bendroflumethiazide was phototoxic at 5 x 10(-5) mol/l and higher concentrations, bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at 2.5 x 10(-4) mol/l and higher concentrations, and the oral antidiabetics glibenclamide and gliquidone as well as the diuretics butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at 5 x 10(-4) mol/l and higher concentrations. The oral antidiabetics chlorpropamide, glipizide, glymidine, tolazamide and tolbutamide as well as the diuretics chlortalidone, furosemide, indapamide and xipamide did not induce phototoxicity in this assay.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9037453&dopt=Abstract
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