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Journal of Pharmacology And Experimental Therapeutics, Vol. 150, Issue 3, 491-498, 1965
Copyright © 1965 by American Society for Pharmacology and Experimental Therapeutics

THE EFFECT OF 5-METHYLPYRAZOLE-3-CARBOXYLIC ACID ON CARBOHYDRATE AND FREE FATTY ACID METABOLISM

George C. Gerritsen 1 and William E. Dulin 1

1 Metabolic Diseases Research, The Upjohn Company, Kalamazoo, Michigan

As a hypoglycemic agent, 5-methylpyrazole-3-carboxylic acid was found to be 116 times more potent orally than tolbutamide in glucose-injected, fasted, intact rats. U-19425 increases glucose oxidation in vivo and in epididymal adipose tissue. It also inhibits the release of free fatty acid (FFA) from adipose tissue in vitro. The pyrazole lowers blood sugar and plasma FFA of eviscerated rats and is effective in decreasing fasting blood sugar levels of alloxan diabetic rats which do not respond to tolbutamide. U-19425 markedly depresses plasma FFA of fasting man.

The data presented suggest that the primary action of U-19425 is on fat metabolism. The data are consistent with the hypothesis that the effect of U-19425 on glucose oxidation and blood sugar depression may be secondary to the initial plasma FFA depression.

Accepted on June 29, 1965






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Copyright © 1965 by the American Society for Pharmacology and Experimental Therapeutics.