Fig. 7.
The cysteinyl leukotriene receptor 1 (CysLT1R) antagonist zafirlukast inhibits volume-regulated anion channel (VRAC). A: structure of zafirlukast. B: zafirlukast concentration-response curve generated from whole cell patch-clamp electrophysiology (mean ± SE IC50 = 17 ± 4 µM; n ≥ 4). C: whole cell currents from human embryonic kidney 293 (HEK293) cells were measured using a ramp protocol from −100 to +100 mV. Cells were exposed to hypotonic bath and hypotonic bath + 30 µM zafirlukast. D: exemplar time course of VRAC activation under hypotonic solution exposure, 30 µM zafirlukast (Z-kast), and wash (hypo) treatment.