FM1-43 dye behaves as a permeant blocker of the hair-cell mechanotransducer channel

J Neurosci. 2001 Sep 15;21(18):7013-25. doi: 10.1523/JNEUROSCI.21-18-07013.2001.

Abstract

Hair cells in mouse cochlear cultures are selectively labeled by brief exposure to FM1-43, a styryl dye used to study endocytosis and exocytosis. Real-time confocal microscopy indicates that dye entry is rapid and via the apical surface. Cooling to 4 degrees C and high extracellular calcium both reduce dye loading. Pretreatment with EGTA, a condition that breaks tip links and prevents mechanotransducer channel gating, abolishes subsequent dye loading in the presence of calcium. Dye loading recovers after calcium chelation with a time course similar to that described for tip-link regeneration. Myo7a mutant hair cells, which can transduce but have all mechanotransducer channels normally closed at rest, do not label with FM1-43 unless the bundles are stimulated by large excitatory stimuli. Extracellular perfusion of FM1-43 reversibly blocks mechanotransduction with half-blocking concentrations in the low micromolar range. The block is reduced by high extracellular calcium and is voltage dependent, decreasing at extreme positive and negative potentials, indicating that FM1-43 behaves as a permeant blocker of the mechanotransducer channel. The time course for the relief of block after voltage steps to extreme potentials further suggests that FM1-43 competes with other cations for binding sites within the pore of the channel. FM1-43 does not block the transducer channel from the intracellular side at concentrations that would cause complete block when applied extracellularly. Calcium chelation and FM1-43 both reduce the ototoxic effects of the aminoglycoside antibiotic neomycin sulfate, suggesting that FM1-43 and aminoglycosides enter hair cells via the same pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoglycosides
  • Animals
  • Anti-Bacterial Agents / pharmacology
  • Calcium / metabolism
  • Cells, Cultured
  • Chelating Agents / pharmacology
  • Dyneins
  • Egtazic Acid / analogs & derivatives
  • Egtazic Acid / pharmacology
  • Extracellular Space / metabolism
  • Fluorescent Dyes / pharmacokinetics
  • Fluorescent Dyes / pharmacology*
  • Hair Cells, Auditory / drug effects*
  • Hair Cells, Auditory / metabolism
  • Heterozygote
  • Homozygote
  • Ion Channels / antagonists & inhibitors*
  • Ion Channels / metabolism
  • Kinetics
  • Mechanoreceptors / drug effects*
  • Mechanoreceptors / metabolism
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Mice
  • Mice, Mutant Strains
  • Myosin VIIa
  • Myosins / deficiency
  • Myosins / genetics
  • Patch-Clamp Techniques
  • Physical Stimulation
  • Pyridinium Compounds / pharmacokinetics
  • Pyridinium Compounds / pharmacology*
  • Quaternary Ammonium Compounds / pharmacokinetics
  • Quaternary Ammonium Compounds / pharmacology*
  • Temperature

Substances

  • Aminoglycosides
  • Anti-Bacterial Agents
  • Chelating Agents
  • FM1 43
  • Fluorescent Dyes
  • Ion Channels
  • Myo7a protein, mouse
  • Myosin VIIa
  • Pyridinium Compounds
  • Quaternary Ammonium Compounds
  • Egtazic Acid
  • Myosins
  • Dyneins
  • 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
  • Calcium