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LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.

LASSBio-1135 (Compound 3a) is an orally active TRPV1 antagonist. LASSBio-1135 is an anti-inflammatory and analgesic compound. LASSBio-1135 inhibits moderately the human PGHS-2 enzyme activity (IC50 = 18.5 μM). LASSBio-1135 reverts the Capsaicin (HY-10448)-induced thermal hyperalgesia and reduces the carrageenan-induced rat paw edem[1].

[1] Lacerda RB, et al. Discovery of novel analgesic and anti-inflammatory 3-arylamine-imidazo[1,2-a]pyridine symbiotic prototypes. Bioorg Med Chem. 2009 Jan 1;17(1):74-84. DOI:10.1016/j.bmc.2008.11.018
[2] Lima CK, et al. LASSBio-1135: a dual TRPV1 antagonist and anti-TNF-alpha compound orally effective in models of inflammatory and neuropathic pain. PLoS One. 2014 Jun 18;9(6):e99510. DOI:10.1371/journal.pone.0099510