Block by extracellular Mg2+ of single human purinergic P2X4 receptor channels expressed in human embryonic kidney cells.

Single channel properties of human P2X4 receptors expressed in human embryonic kidney cells have been investigated by outside-out mode patch clamp recordings. P2X4 channel activity was characterized by very fast kinetics. The current-voltage relationship was strongly non-linear at potentials <-100 mV. A slope conductance of approximately 9 pS was estimated at the approximately linear part of the current-voltage relation (>-100 mV). External Mg2+ reversibly decreased the amplitude of ATP-evoked single channel currents in a concentration-dependent manner but independent of the membrane potential. Additionally, extracellular Mg2+ shortened the mean open time whereas the mean closed time was not affected. Thus, Mg2+ ions are proposed to inhibit the function of human P2X4 receptors by means of an open-channel block with a Mg2+ binding site at the exterior surface of the pore.