Eliprodil stimulates CNS myelination: new prospects for multiple sclerosis?

Neurology. 1999 Jan 15;52(2):346-50. doi: 10.1212/wnl.52.2.346.

Abstract

Objective: To examine the potential of eliprodil-a neuroprotective agent with a high affinity for sigma-receptors-to promote myelination in neuron-oligodendrocytes cocultures.

Background: Remyelination is one of the major therapeutic issues in MS. Because neuronal integrity is required for CNS myelination, the authors postulated that neuroprotective molecules might favor myelination.

Methods: Two experimental culture conditions were compared: standard medium Bottenstein and Sato ([B-S] medium) and a medium depleted of both thyroid hormones and progesterone (depleted [D] medium). Myelination was quantified by counting the number of myelinated internodes, identified immunocytochemically with an antimyelin basic protein (anti-MBP) antibody.

Results: The authors first confirmed that in D medium myelination was reduced by a factor of 3.5 compared with cultures maintained in B-S medium. Under both culture conditions, addition of 10(-6) M eliprodil did not modify significantly the total number of either microtubule associated protein-2-positive neurons or MBP-positive oligodendrocytes. However, eliprodil induced a twofold (p < 0.01) increase in myelination when added to B-S medium, and a 4.7-fold (p < 0.0001) increase when added to D medium.

Conclusion: Although the molecular mechanism mediating the effect of the sigma-receptor agonist on myelination remains to be elucidated, these results strongly suggest that neuroprotective molecules may be of therapeutic interest in demyelinating diseases such as MS.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Axons / drug effects
  • Central Nervous System / cytology
  • Central Nervous System / drug effects*
  • Coculture Techniques
  • Drug Evaluation, Preclinical
  • Forecasting
  • Mice
  • Multiple Sclerosis / drug therapy*
  • Myelin Sheath / drug effects*
  • Neurons / drug effects
  • Neurons / ultrastructure
  • Neuroprotective Agents / therapeutic use*
  • Oligodendroglia / drug effects
  • Oligodendroglia / ultrastructure
  • Piperidines / therapeutic use*
  • Receptors, sigma / drug effects*
  • Stimulation, Chemical
  • Triiodothyronine / pharmacology

Substances

  • Neuroprotective Agents
  • Piperidines
  • Receptors, sigma
  • Triiodothyronine
  • eliprodil