Pharmacological characterization of [3H]MK-801 binding in the rat spinal cord

Eur J Pharmacol. 1996 Jul 4;307(3):347-53. doi: 10.1016/0014-2999(96)00273-7.

Abstract

Using a receptor binding assay for [3H](+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-10-imi ne (MK-801) the pharmacology of spinal cord NMDA receptors was compared to that of NMDA receptors in the cerebral cortex. The affinities of glutamate site agonists L-glutamate, L-aspartate, ibotenic acid, NMDA and quinolinic acid for stimulation of [3H]MK-801 binding were 6-10 times lower in the spinal cord and the efficacy of quinolinic acid was 50% of that of the other agonists in this region. Also the affinities of glycine site agonists glycine, D-serine, D-alanine and L-serine were lower in the spinal cord as were the affinities of the non-competitive antagonists phencyclidine, (+/-)-cyclazocine and dextromethorphan. The divalent cations Zn2+, Mg2+ and Ca2+ had 4-8 times lower affinity for spinal NMDA receptors while the affinity of Co2+ was 50 times lower. The affinity of [3H]MK-801 was 2.5-fold lower in the spinal cord. These data show that spinal cord NMDA receptors show qualitative and quantitative differences compared to those in the cerebral cortex.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids, Dicarboxylic / pharmacology*
  • Animals
  • Binding, Competitive
  • Cations, Divalent
  • Cerebral Cortex / metabolism
  • Dizocilpine Maleate / metabolism*
  • Excitatory Amino Acid Agonists / metabolism
  • Excitatory Amino Acid Antagonists / metabolism*
  • Glutamic Acid / metabolism
  • Glycine / metabolism
  • In Vitro Techniques
  • Male
  • Protein Binding / drug effects
  • Radioligand Assay
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Receptors, N-Methyl-D-Aspartate / drug effects
  • Receptors, N-Methyl-D-Aspartate / metabolism*
  • Spinal Cord / metabolism*

Substances

  • Amino Acids, Dicarboxylic
  • Cations, Divalent
  • Excitatory Amino Acid Agonists
  • Excitatory Amino Acid Antagonists
  • Receptors, N-Methyl-D-Aspartate
  • (alpha-carboxycyclopropyl)glycine
  • Glutamic Acid
  • Dizocilpine Maleate
  • Glycine