Reference

Glibenclamide is exceptional among hypoglycemic sulfonylureas in accumulating progressively in b-cell-rich pancreatic islets

Glibenclamide is exceptional among hypoglycemic sulfonylureas in accumulating progressively in b-cell-rich pancreatic islets. Hellman, Bo; Sehlin, Janove; Taeljedal, Inge Bert (Dep. Med. Cell Biol., Univ. Uppsala, Uppsala S-751 23, Swed.). Acta Endocrinol. (Copenhagen), 105(3), 385-90 (English) 1984. CODEN: ACENA7. ISSN: 0001-5598. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Six hypoglycemic sulfonylurea compds. were compared with regard to their ability to bind to b-cell rich pancreatic islets microdissected from ob/ob mice. Glibenclamide (I) [10238-21-8] differed from carbutamide [339-43-5], tolbutamide [64-77-7], chlorpropamide [94-20-2], glibornuride [26944-48-9] and glipizide [29094-61-9] in not being rapidly bound to an equil., but accumulating progressively in amts. far exceeding the water space. An inhibitor of the anion channels in the b-cell membrane, 4-acetamido-4'-isothiocyanatestilbene-2,2'-disulfonic acid (SITS), suppressed the islet uptake of glibenclamide and to some extent also that of carbutamide and glibenclamide. The unusual uptake characteristics of glibenclamide had their counterpart in a retardation of its max. 35207-08-0 and 339-43-5 are just another two chemicals used in this study. action in promoting the entry of Ca2+ into the b-cells. .

Adsorption of sulfonylureas onto activated charcoal in vitro

Adsorption of sulfonylureas onto activated charcoal in vitro. Kannisto, Hannu; Neuvonen, Pertti J. (Dep. Clin. Pharmacol., Univ. Helsinki, Helsinki SF-00250/25, Finland). J. Pharm. Sci., 73(2), 253-6 (English) 1984. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 4 Adsorption of carbutamide [339-43-5], chlorpropamide [94-20-2], tolazamide [1156-19-0], tolbutamide [64-77-7], glibenclamide [10238-21-8], and glipizide [29094-61-9] onto activated charcoal was compared in vitro using different charcoal-to-drug ratios. Maximal binding capacities of different sulfonylureas were 0.45-0.52 g/g of charcoal at pH 7.5. The affinity of the 2nd-generation derivs., glibenclamide and glipizide, was considerably higher than that of the 1st-generation derivs. The affinity of sulfonylureas to charcoal was higher at pH 4.9 than at pH 7.5.In this experiment, several chemicals are used like 94-20-2 and 10238-21-8 Poor water soly. of sulfonylureas at pH 1 prevents the adequate testing in these conditions. Contrary to what has appeared previously, activated charcoal effectively adsorbs different sulfonylureas and possibly can be used to prevent their gastrointestinal absorption. .