LASSBio-1135

LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.Oral administration of 100 mol x Kg (-1) LASSBio-1135 markedly reduced thermal hyperalgesia induced by carrageenan, however at 10 mol x Kg (-1) only a partial reduction was observed at the 4th h. Neutrophil recruitment and TNF-α production after carrageenan stimulus was also inhibited by the treatment with LASSBio-1135. Modulating TRPV1 and TNF-α production, two key therapeutic targets of neuropathic pain, 100 mol x Kg (-1) LASSBio-1135 was orally efficacious in reversing thermal hyperalgesia and mechanical allodynia produced by partial sciatic ligation 7-11 days after surgery without provoking hyperthermia, a common side effect of TRPV1 antagonists.