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FPR agonists and antagonists act on formyl peptide receptors (FPRs) of innate immune cells. Humans express three of these G protein-coupled receptors, FPR1, FPR2 and FPR3, and FPR2 is also known as the lipoxin A4 receptor (ALX) because it binds this lipid mediator. FPR1 recognizes N-formylated peptides released by bacteria and damaged mitochondria and directs neutrophil chemotaxis and activation. FPR2 binds a wider range of peptide and lipid ligands and is studied in the resolution of inflammation. HCH6-1 and cyclosporin H are FPR1 antagonists, whereas ACT-389949, BMS-986235 and BMS-986331 activate FPR2. The synthetic hexapeptide WKYMVm TFA and FPR Agonist 43 stimulate both FPR1 and FPR2.
Cyclosporin H is a TPA/PMA inhibitor and a selective inhibitor of formyl peptide receptors (Ki = 0.1 uM).
FPR1 Antagonist 3 is a potent and selective inhibitor of the formyl peptide receptor 1 (FPR1). It effectively inhibits superoxide anion generation and elastase release, with IC50 values of 0.33 μM and 0.84 μM, respectively. This compound is valuable for research applications aimed at investigating inflammatory responses and receptor signaling pathways related to FPR1 activity.
