Fig. 2.

The novel TRPV4 blocker GSK2334775 potently blocks TRPV4-containing channels in vitro and inhibits GSK1016790A-induced constriction of the human bronchus. (A) Chemical structure of GSK2334775 (see the text for full chemical name). (B) Summary data demonstrating the inhibition of the GSK1016790A-induced Ca²⁺ mobilization in human attachment-selected BAL cells by GSK2334775 (▪, control; ▴, 10 nM; ▾, 100 nM), and its abolition by ruthenium red (♦, 10 μM, mean ± S.E.M. of 3–5 experiments). (C) Summary data demonstrating that GSK1016790A-dependent contractions of human bronchi are inhibited in a concentration-dependent manner by the novel TRPV4 blocker GSK2334775 (mean ± S.E.M. of five to six experiments). Asterisks denote statistically significant differences from the control (P < 0.05, one-way analysis of variance with Dunnett’s multiple comparison test).