Inhibition of 3H-glibenclamide binding to sulfonylurea receptors by oral antidiabetics.
Specific binding of 3H-glibenclamide (HB 419) is observed with membranes from rat cerebral cortex and rat beta-cell tumor. 3H-Glibenclamide binding is of high affinity, reversible, saturable, and can be displaced by oral antidiabetics of different structural types. Half maximal inhibition of binding correlates with the hypoglycemic action of the compounds.
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001786:Blood Glucose / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D005260:Female; D005905:Glyburide / Q000378:metabolism*; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D007340:Insulinoma / Q000378:metabolism; D008297:Male; D008566:Membranes / Q000378:metabolism; D009368:Neoplasm Transplantation; D010190:Pancreatic Neoplasms / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug / Q000378:metabolism*; D013453:Sulfonylurea Compounds / Q000378:metabolism*
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D011955:Receptors, Drug; D013453:Sulfonylurea Compounds; D005905:Glyburide