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. 2017 Mar 10;25(5):471–481. doi: 10.4062/biomolther.2016.096

Table 3.

The essential information about inhibitors of TRPC channels or interdependent channels.

Inhibitor Chemical structure Targeting channels Predicted effects Action mechanism Reference
SKF96365 graphic file with name bt-25-471i1.jpg TRPC1, TRPC2, TRPC3, TRPC4, TRPC5, TRPC6, TRPC7 Selectively decrease receptor-mediated calcium entry (RMCE) in human platelets, neutrophils and endothelial cells Inhibit receptor-mediated Ca2+ entry and voltage-gated Ca2+ entry Merritt et al., 1990; Farooqi et al., 2013
Pyrazole-3 (Pyr3) graphic file with name bt-25-471i2.jpg TRPC3 Prevent stent-induced arterial remodeling and inhibit SMC proliferation Inhibit TRPC3 by binding to the extracellular side of the receptor Rowell et al., 2010; Christian and Maik, 2011; Koenig et al., 2013
SAR7334 graphic file with name bt-25-471i3.jpg TRPC3, TRPC6, TRPC7 Effect on acute hypoxic pulmonary vasoconstriction and systemic blood pressure Inhibit TRPC3, TRPC6, TRPC7-mediated Ca2+ influx into cells Maier et al., 2015
GsMTx-4 Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-Asp-Asp-Lys-Cys-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe-NH2 Stretch-activated ion channels and NaV1.7 Na + channels and TRPC1, TRPC6 Potential therapeutic targets for cardiac arrhythmias Inhibit Na+ voltage-gated channels and cation-selective mechanosensitive channels Franz and Bode, 2003; Bowman et al.,2007; Rowell et al., 2010
BTP2 graphic file with name bt-25-471i4.jpg TRPCs and Store-operated Ca2+ influx and Ca2+ release-activat ed Ca2+ channels Suppresses cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and proliferation in T cells in vitro Inhibit anti-CD3 antibody-induced sustained Ca2+ influx Ohga et al., 2008; Rowell et al., 2010