N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad-spectrum phospholipase A2 (PLA2) inhibitor and TRP channel blocker [1] [2].
PLA2 enzymes are a family of structurally different enzymes including at least nine subfamilies. The mammalian TRP proteins including at least 27 members and can be grouped into TRPC, TRPV, TRPM, TRPA, TRPP, and TRPML six subfamilies [1].
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad-spectrum PLA2 inhibitor and TRP channel blocker [1] [2]. In HEK293 cells transfected with human TRPM2, ACA (20 ?M) completely blocked H2O2-induced Ca2+ signals and ADPR-induced whole-cell currents with IC50 value of 1.7 ?M. ACA (20 ?M) also blocked human TRPM8-induced Ca2+ signals and TRPC6-mediated currents with IC50 values of 3.9 ?M and 2.3 ?M, respectively. ACA can serve as a useful tool for studying the function of TRPM2 in native cells [2]. In isolated pig cardiac ventricular myocytes, ACA reversibly inhibited ICl(Ca) with IC50 value of 4.2 ?M in a concentration-dependent way. ACA (50 ?M) also inhibited the cAMP-activated chloride current.
References:
[1].Harteneck C, Frenzel H, Kraft R. N-(p-amylcinnamoyl)anthranilic acid (ACA): a phospholipase A(2) inhibitor and TRP channel blocker. Cardiovasc Drug Rev. 2007 Spring;25(1):61-75.
[2].Kraft R, Grimm C, Frenzel H, et al. Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid. Br J Pharmacol. 2006 Jun;148(3):264-73.
[3].Gwanyanya A, Macianskiene R, Bito V, et al. Inhibition of the calcium-activated chloride current in cardiac ventricular myocytes by N-(p-amylcinnamoyl)anthranilic acid (ACA). Biochem Biophys Res Commun. 2010 Nov 19;402(3):531-6.