219680-33-8Relevant academic research and scientific papers
Glucagon antagonists/inverse agonists
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, (2008/06/13)
Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
Identification of alkylidene hydrazides as glucagon receptor antagonists
Ling,Hong,Gonzalez,Gregor,Polinsky,Kuki,Shi,Teston,Murphy,Porter,Kiel,Lakis,Anderes,May,Knudsen,Lau
, p. 3141 - 3149 (2007/10/03)
High throughput screening of our small molecule combinatorial library identified a class of benzoylnaphthalenehydrazones with modest affinity for the human glucagon receptor. Optimization of this initial hit through a series of targeted libraries and traditional medicinal chemistry led to ligands with nanomolar affinities. Pharmacological evaluation demonstrated that these ligands were competitive glucagon receptor antagonists. Intravenous administration of a representative benzoylnaphthalenehydrazone into rats attenuated glucagon-stimulated glucose levels.
