Advances in non-peptide glucagon receptor antagonists

Curr Pharm Des. 1999 Sep;5(9):683-691.

Abstract

This review deals with glucagon receptor antagonism as a possible treatm ent 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 immunone utralisation suggests that glucagon plays a modest (rats) to substantial (rabbits) role in the maintenance of euglycaemia and is an important dia betogenic factor. These data strongly suggest that glucagon antagonism may be a beneficial and safe therapeutic approach for the treatment of T ype 2 diabetes. Further, the progress on non-peptide glucagon receptor antagonists is reviewed with special focus on the different classes of g lucagon receptor antagonists published, namely quinoxalines /pyrrolo[1,2 -a]quinoxalines, mercaptobenzimidazoles, 2-pyridyl-3,5-diarylpyrroles, q uinoline hydrazones, 4-phenylpyridines, and alkylidene hydrazides.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies / physiology
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Disease Models, Animal
  • Hypoglycemic Agents / pharmacology*
  • Peptides / pharmacology*
  • Receptors, Glucagon / antagonists & inhibitors*

Substances

  • Antibodies
  • Hypoglycemic Agents
  • Peptides
  • Receptors, Glucagon