Inhibition of 3H-glibenclamide Binding to Sulfonylurea Receptors by Oral Antidiabetics

Overview

Journal Arzneimittelforschung

Specialty Pharmacology

Date 1985 Jan 1

PMID 3925960

Citations 14

Authors

K Geisen

V Hitzel

R Okomonopoulos

J Punter

R Weyer

H D SUMM

Affiliations

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Abstract

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.

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Bernardi H, Fosset M, Lazdunski M Proc Natl Acad Sci U S A. 1988; 85(24):9816-20.

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