LF22-0542

LF22-0542

Names
IUPAC name N-[[4-(4,5-Dihydro-1H-imidazol-2-yl)phenyl]methyl]-2-[2-[[(4-methoxy-2,6-dimethylphenyl) sulfonyl]methylamino]ethoxy]-N-methylacetamide
Identifiers
CAS Registry Number	633698-99-4 Y
Jmol-3D images	Image
SMILES COC1=CC(C)=C(S(N(C)CCOCC(N(C)CC2=CC=C(C3=NCCN3)C=C2)=O)(=O)=O)C(C)=C1
Properties
Chemical formula	C25H34N4O5S
Molar mass	502.63 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

LF22-0542 is a non-peptide bradykinin B₁ antagonist. It displayed binding Ki values of 0.35 and 6.5 nM at cloned human and mouse B₁ receptors, respectively, while having no affinity for either human, mouse, or rat B₂ receptors at concentrations up to 10 μM. This means that LF22-0542 is at least 4000 times selective for the B₁ receptor over the B₂ receptor. Systemic administration of LF22-0542 inhibited acute pain induced by acetic acid, formalin, and a hot plate. It also reversed acute inflammatory pain induced by carrageenan, and persistent inflammatory pain induced by CFA. In a neuropathic pain model, LF22-0542 reversed the thermal hyperalgesia, but not the mechanical hyperalgesia.