Effect of linogliride on hormone release from perfused rat pancreas. Fuel dependence and desensitization by tolbutamide

• Published in: Diabetes (New York, N.Y.) Vol. 40; no. 7; pp. 878 - 884
• Main Authors: Ronner, P., Cheong, E., Khalid, P., Tuman, R. W., Matschinsky, F. M.
• Format: Journal Article
• Language: English
• Published: American Diabetes Association 01-07-1991
• ISSN: 0012-1797; 1939-327X; 0012-1797
• DOI: 10.2337/diabetes.40.7.878

Effect of linogliride on hormone release from perfused rat pancreas. Fuel dependence and desensitization by tolbutamide.
P Ronner ,
E Cheong ,
P Khalid ,
R W Tuman and
F M Matschinsky
Department of Biochemistry and Biophysics, School of Medicine, University of Pennsylvania, Philadelphia 19104-6015.
Abstract
We examined the effect of the hypoglycemic drug linogliride on hormone release from the in vitro perfused rat pancreas. Linogliride
stimulated insulin release in the absence of glucose either in the presence or absence of a physiological mixture of amino
acids. In addition, linogliride inhibited amino acid-induced glucagon release. Half-maximal effects of linogliride on insulin
and glucagon release were achieved at concentrations as low as 26 and 3 microM, respectively. The effects of linogliride on
hormone release largely resembled those of tolbutamide. In the absence of amino acids, the stimulation of insulin release
by linogliride or tolbutamide was transient. When the pancreas had been preperfused for 20 min with tolbutamide, linogliride
no longer had an effect on hormone release. Likewise, tolbutamide remained without effect in pancreases preperfused with linogliride.
These data suggest that linogliride and tolbutamide may have a similar mechanism of action.