(-)-Ephedrine has been used in the treatment of patients with myasthen
ia gravis. To investigate the possible effects of ephedrine on neuromu
scular transmission, canine intercostal muscle endplates were studied
by microelectrode techniques. At concentrations less than 10(-4) M, ep
hedrine had no effect on neuromuscular transmission. At a concentratio
n of 10(-4) M, ephedrine increased the quantal content of the endplate
potential by 21%. The presynaptic store of acetylcholine quanta avail
able for immediate release was unchanged, but the probability of quant
al release was increased by 16%. At this concentration, ephedrine decr
eased the amplitude of the miniature endplate potential by 38%. In the
presence of 10(-3) M ephedrine, the miniature endplate potentials and
currents became undetectable. The kinetic properties of the acetylcho
line receptor channel were studied by analysis of acetylcholine-induce
d endplate current noise. At 10(-4) M , ephedrine reduced the channel
conductance by 43% but had no effect on the open time. At 5 x 10(-4) M
, ephedrine reduced the channel conductance by 84% and increased the o
pen time by 23 percent.