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Published in

Bentham Science Publishers, Current Pharmaceutical Design, 9(5), p. 683-691, 1999

DOI: 10.2174/1381612805666230111194905

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Advances in Non-Peptide Glucagon Receptor Antagonists

Journal article published in 1999 by P. Madsen, C. L. Brand ORCID, J. J. Holst, J. J. Holste, L. B. Knudsen
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

This review deals with glucagon receptor antagonism as a possible treatment of Type 2 diabetes. The role of glucagon in animal models has been studied by glucagon antibodies as model antagonists. Depending upon the animal model studied, selective glucagon deficiency produced by immunoneutralisation suggests that glucagon plays a modest (rats) to substantial (rabbits) role in the maintenance of euglycaemia and is an important diabetogenic factor. These data strongly suggest that glucagon antagonism may be a beneficial and safe therapeutic approach for the treatment of Type 2 diabetes. Further, the progress on non-peptide glucagon receptor antagonists is reviewed with special focus on the different classes of glucagon receptor antagonists published, namely quinoxalines / pyrrolo[l ,2-a]quinoxalines, mercaptobenzimidazoles, 2-pyridyl-3,5-diarylpyrroles, quinoline hydrazones, ·4.-phenylpyridines, and alkylidene hydrazides.