Nomenclature	http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=710
Activators	http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4207
Endogenous channel blockers	intracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=708, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2391
Channel blockers	http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4100, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4113, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4174, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4177, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4217, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4270, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4273, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4151, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4159, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4176, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4204, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4252, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2522, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4263, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4265, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2342, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2510, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1016
Functional Characteristics	γ = 10–20 pS (negative potentials), 50–90 pS (positive potentials); permeability sequence SCN > I > NO3 ‐ >Br‐ > Cl‐ > F‐ > gluconate; outward rectification due to voltage dependence of γ; inactivates at positive potentials in many, but not all, cell types; time dependent inactivation at positive potentials; intracellular ionic strength modulates sensitivity to cell swelling and rate of channel activation; rate of swelling‐induced activation is modulated by intracellular ATP concentration; ATP dependence is independent of hydrolysis and modulated by rate of cell swelling; inhibited by increased intracellular free Mg2+ concentration; swelling induced activation of several intracellular signalling cascades may be permissive of, but not essential to, the activation of VRAC including: the Rho‐Rho kinase‐MLCK; Ras‐Raf‐MEK‐ERK; PIK3‐NOX‐H2O2 and Src‐PLCγ‐Ca2+ pathways; regulation by PKCα required for optimal activity; cholesterol depletion enhances activity; activated by direct stretch of β1‐integrin
Comments	VRAC is also activated by cell swelling and low intracellular ionic strength. VRAC is also blocked by chromones, extracellular nucleotides and nucleoside analogues