LHRH and GTP-γ-S modify calcium current activation in bullfrog sympathetic neurons

LHRH (chicken II luteinizing hormone-releasing hormone) partially reduces calcium currents and slows the activation kinetics of part of the remaining current in frog sympathetic neurons. The effects of LHRH are mimicked by intracellular dialysis with GTP-γ-S. A strong depolarization can temporarily reverse the effects of LHRH or GTP-γ-S: activation kinetics return to normal, and the amplitude of the current is increased (facilitation). Facilitation develops rapidly (π = 4–6 ms at >+30 mV) and decays more slowly ( t 1 2 = 60 ms at −80 mV). Tail currents in LHRH are smaller and faster than in the control, and these effects are partially reversed by facilitation. These results can be explained by a model in which a fraction of the channels is shifted into a “reluctant” gating mode, where opening requires stronger depolarization. If this mechanism is at the root of presynaptic inhibition, our results predict that inhibition of transmitter release would be overcome during bursts of high frequency activity.