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Background and purpose:  Compound LASSBio‐881 is an orally effective antinociceptive that binds to cannabinoid receptors and is active mainly on the neurogenic component of pain models. We investigated whether transient receptor potential vanilloid subfamily type 1 (TRPV1) channels are involved in the effects of LASSBio‐881.

Experimental approach:  Modulation of capsaicin (CAP)‐ and low pH‐induced currents was evaluated in TRPV1‐expressing Xenopus oocytes. In vivo effects were evaluated in CAP‐induced acute and inflammatory changes in nociception, as well as in partial sciatic ligation‐induced thermal hypernociception.

Key results:  LASSBio‐881 inhibited TRPV1 currents elicited by CAP with an IC₅₀ of 14 µM, and inhibited proton‐gated currents by 70% at 20 µM. Functional interaction with CAP was surmountable. Locally applied LASSBio‐881 decreased time spent in CAP‐elicited …