Binding of tetrodotoxin and saxitoxin to Na+ channels at different holding potentials: fluctuation measurements in frog myelinated nerve

Biochim Biophys Acta. 1989 Oct 16;985(2):161-7. doi: 10.1016/0005-2736(89)90361-1.

Abstract

The number of available Na+ channels in nodes of frog nerve fibres was determined from nonstationary Na+ current fluctuations recorded during a train of depolarizing test pulses. Mean numbers in Ringers's solution were 90,000 at a hyperpolarizing holding potential VH = -40 mV, 50,000 at the resting potential (VH = 0 mV) and 30,000 at a depolarizing holding potential VH = 30 mV. Addition of the cationic channel blockers tetrodotoxin (TTX) or saxitoxin (STX) to Ringer reduced the channel number by a factor which was independent of the holding potential. The reduction factor was 4 for 9.3 nM TTX and 3 for 3.5 nM STX. Thus, in the state of repetitive stimulation, TTX or STX blockage of Na+ channels is hardly affected by the membrane potential. Taking into account use-dependent TTX and STX effects [1], it is concluded that binding of both toxins exhibits a weak voltage dependence with toxin affinities decreasing at more negative holding potentials. The results suggest that binding of TTX and STX occurs at an external superficial receptor near the Na+ channel and that the toxin affinity of the receptor may be modulated by fast Na+ activation and slow inactivation gating processes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Kinetics
  • Membrane Potentials
  • Nerve Fibers, Myelinated / metabolism
  • Nerve Fibers, Myelinated / physiology*
  • Rana esculenta
  • Saxitoxin / metabolism*
  • Sodium / metabolism
  • Sodium Channels / metabolism
  • Sodium Channels / physiology*
  • Tetrodotoxin / metabolism*

Substances

  • Sodium Channels
  • Saxitoxin
  • Tetrodotoxin
  • Sodium