2-APB activates TRPV1, TRPV2 and TRPV3 but not TRPV4, TRPV5 and TRPV6. It blocks TRPC5 (IC50=20µM), TRPC6, TRPM3 and TRPM8. It potentiates the effect of capsaicin, protons and heat on TRPV1. It was originally introduced as an IP3 receptor blocker and subsequently as an inhibitor of store-operated Ca2+ entry (75 µM).
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