Safotibant (INN) also known by the research code LF22-0542 is a non-peptide bradykinin B₁

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

. 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 Acetic acid , systematically named ethanoic acid , is an acidic, colourless liquid and organic compound with the chemical formula (also written as , , or ). Vinegar is at least 4% acetic acid by volume, making acetic acid the main component ...

, 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.

References

{{Reflist Analgesics Anti-inflammatory agents Sulfonamides Imidazolines Carboxamides Ethanolamines Methoxy compounds