Figure 3
From: Reactive metabolites of acetaminophen activate and sensitize the capsaicin receptor TRPV1
Activation of TRPV1 by pBQ does not involve the capsaicin-binding domain or proteinkinase C-dependent phosphorylation. pBQ (1 µM, 1.5–2 min) sensitized voltage ramp-induced currents in rTRPV1 (A) and oTRPV1 (B), the latter suggesting a mechanism independent of the capsaicin-binding site. (C) Sensitization of hTRPV1 by pBQ (1 µM, 2 min) is additive to sensitization by PKC-dependent phosphorylation evoked by PMA (300 nM). (D) In an rTRPV1 mutant lacking the PKC-phosphorylation site S800, membrane currents are still clearly sensitized by pBQ (1 µM 2–3 min).
