Key result
The small-molecule AT2 receptor agonist compound 21 (C21) demonstrated high affinity for the AT2R (Ki = 0.4 nM) and provides a scaffold for exploring structure-activity relationships.
Compound 21 is a highly selective small-molecule AT2 receptor agonist that serves as a valuable tool for studying AT2R pharmacology.
The discovery of the first selective, small‐molecule ATR receptor (AT2R) agonist compound 21 (C21) ( 8 ) that is now extensively studied in a large variety of in vitro and in vivo models is described. The sulfonylcarbamate derivative 8 , encompassing a phenylthiofen scaffold is the drug‐like agonist with the highest affinity for the AT2R reported to date ( K i = 0.4 nM). Structure‐activity relationships (SAR), regarding different biaryl scaffolds and functional groups attached to these scaffolds and with a particular focus on the impact of various para substituents displacing the methylene imidazole group of 8 , are discussed. Furthermore, the consequences of migration of the methylene imidazole group and presumed structural requirements for ligands that are aimed as AT2R agonists (e.g. 8 ) or AT2R antagonists (e.g. 9 ), respectively, are briefly addressed. A summary of the pharmacological actions of C21 ( 8 ) is also presented.
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Hallberg et al. (2017) reported a review. Compound 21 (C21) was evaluated. The small-molecule AT2 receptor agonist compound 21 (C21) demonstrated high affinity for the AT2R (Ki = 0.4 nM) and provides a scaffold for exploring structure-activity relationships.
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