Acamprosate inhibits Ca2+ influx mediated by NMDA receptors and voltage-sensitive Ca2+ channels in cultured rat mesencephalic neurones

Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):440-3. doi: 10.1007/s002100000285.

Abstract

Acamprosate has recently been introduced in relapse prophylaxis in weaned alcoholics. Using fura-2 microfluorimetry, the present study investigates whether acamprosate affects N-methyl-D-aspartate (NMDA) or K+-induced changes in free intracellular Ca2+ concentration ([Ca2+]i) in rat cultured mesencephalic neurones. Both application of NMDA (plus glycine) and elevation of extracellular K+ induced rapid increases in [Ca2+]i which respectively were insensitive and sensitive to omega-conotoxin (omega-CTX) MVIIC, a blocker of voltage-dependent Ca2+ channels (VDCCs). Acamprosate (100 microM and 300 microM) significantly attenuated the response induced by NMDA as well as that induced by K+ in a concentration-dependent manner. Concurrent application of omega-CTX MVIIC and acamprosate impaired the K+-induced increase in [Ca2+]i to the same extent as omega-CTX MVIIC alone. The present data suggest that acamprosate inhibits Ca2+ influx through both NMDA receptors and VDCCs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acamprosate
  • Alcohol Deterrents / pharmacology*
  • Animals
  • Calcium / metabolism*
  • Calcium Channels / physiology*
  • Cells, Cultured
  • Mesencephalon / drug effects*
  • Mesencephalon / metabolism
  • Neurons / drug effects*
  • Neurons / metabolism
  • Rats
  • Receptors, N-Methyl-D-Aspartate / physiology*
  • Taurine / analogs & derivatives*
  • Taurine / pharmacology*
  • omega-Conotoxins / pharmacology

Substances

  • Alcohol Deterrents
  • Calcium Channels
  • Receptors, N-Methyl-D-Aspartate
  • omega-Conotoxins
  • omega-conotoxin-MVIIC
  • Taurine
  • Acamprosate
  • Calcium