402832-51-3Relevant academic research and scientific papers
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists
Chen, Chen,Yu, Jinghua,Fleck, Beth A.,Hoare, Sam R. J.,Saunders, John,Foster, Alan C.
, p. 4083 - 4088 (2004)
A series of phenylguanidine analogues represented by 10, 12, and 21 were synthesized and found to have high binding affinities for the human melanocortin-5 receptor. Their binding affinities for three other melanocortin receptor subtypes, MC1, MC3, and MC4, were low. Selected compounds were also tested for their functional activity and exhibited inhibition of α-MSH-stimulated cAMP production in cells expressing the human MC5 receptor. Compound 10 had a Ki value of 2.1 nM in the binding assay and an IC50 of 72 nM in the functional assay. Some analogues such as 13 from this series possessed weak agonist activity at the human MC4 receptor.
