Detailed analysis of biased histamine<scp>H</scp><scp>₄</scp>receptor signalling by<scp>JNJ</scp>7777120 analogues

Abstract

Small structural modifications resulted in diverse intrinsic activities for unbiased (75) and β-arrestin2-biased indolecarboxamides. Analysis of ligand and receptor features revealed efficacy hotspots responsible for biased-β-arrestin2 recruitment. This knowledge is useful for the design of hH₄R ligands with biased intrinsic activities and aids our understanding of the mechanism of H₄R activation.