SB-452533 acts as a competitive inhibitor at the capsaicin binding site on the transient receptor potential channel TRPV1 receptor with a pKb of 7.7 versus capsaicin and pIC50 of 7.0 versus pH. At higher concentrations, SB-452533 is also active at TRPM8 with an IC50 of 571 nM. It has a high clearance rate, so is not suitable for in vivo use.
SB-452533 acts as a competitive inhibitor at the capsaicin binding site on the transient receptor potential channel TRPV1 receptor.
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