Effect of sodium ion on the affinity of naloxone for the kappa opioid receptor

Life Sci. 1987 Mar 16;40(11):1071-4. doi: 10.1016/0024-3205(87)90569-8.


Several investigators have observed that sodium ion enhances the binding of naloxone to opioid receptors. This effect has generally been attributed to allosteric modulation of the state of the mu receptor. However, a recent claim has been made that the enhancement does not involve a change in the mu receptor, but instead occurs because naloxone becomes a more kappa-specific drug when sodium ion is present in high concentration. Since the claim was not based on experimental evidence from binding studies involving known high-affinity kappa ligands, we have investigated the competition of naloxone for the kappa site using [3H]U-69593 as the marker for receptor binding. Assays were carried out in the presence and absence of 100 mM NaCl. The results of the study indicate that sodium ion does not increase the affinity of naloxone or U-69593 for the kappa receptor.

MeSH terms

  • Animals
  • Benzeneacetamides*
  • Binding, Competitive
  • Brain / metabolism*
  • Cations, Monovalent
  • Cell Membrane / metabolism
  • Guinea Pigs
  • Naloxone / metabolism*
  • Pyrrolidines / metabolism
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, kappa
  • Sodium / pharmacology*


  • Benzeneacetamides
  • Cations, Monovalent
  • Pyrrolidines
  • Receptors, Opioid
  • Receptors, Opioid, kappa
  • Naloxone
  • Sodium
  • U 69593