The polyamine diaminodecane (DA-10) produces a voltage-dependent flickery block of single NMDA receptor channels

Neurosci Lett. 1992 Sep 14;144(1-2):111-5. doi: 10.1016/0304-3940(92)90728-p.


Receptor binding assays have shown that diaminodecane (DA-10) reduced binding of open channel blockers to the N-methyl-D-aspartate (NMDA) subtype of postsynaptic glutamate receptor through an interaction with the polyamine regulatory site. Because the action of DA-10 was opposite to that of the polyamine agonist spermine and was reversed by polyamine antagonists, DA-10 has been classified as an inverse agonist at the polyamine site. Using whole-cell voltage-clamp and single-channel recordings from cultured rat cortical neurons, we show that at negative holding potentials DA-10 (1-300 microM) reduced NMDA receptor whole cell current (IC50 = 34 microM) and produced a flickery block of NMDA single-channel currents. The flickery block of NMDA single channels was voltage-dependent and not reversed by the polyamine antagonist diethylenetriamine (DET). Potential mechanisms for the flickery block of NMDA single channel currents are discussed.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Diamines / pharmacology*
  • Female
  • Ion Channels / drug effects*
  • Kinetics
  • N-Methylaspartate / pharmacology
  • Neurons / drug effects
  • Neurons / metabolism
  • Oocytes / metabolism
  • Polyamines / pharmacology
  • Pregnancy
  • Rats
  • Receptors, N-Methyl-D-Aspartate / drug effects*
  • Spermine / pharmacology


  • 1,10-diaminodecane
  • Diamines
  • Ion Channels
  • Polyamines
  • Receptors, N-Methyl-D-Aspartate
  • diethylenetriamine
  • Spermine
  • N-Methylaspartate