CPP, a new potent and selective NMDA antagonist. Depression of central neuron responses, affinity for [3H]D-AP5 binding sites on brain membranes and anticonvulsant activity

Brain Res. 1986 Sep 10;382(1):169-73. doi: 10.1016/0006-8993(86)90127-7.

Abstract

Properties of a new potent antagonist acting selectively at N-methyl-D-aspartate (NMDA) type excitatory amino acid receptors are described. This compound, 3-((+/-)-2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) is more potent than all previously reported NMDA antagonists in depressing mammalian spinal neuronal responses (cat and immature rat), in its affinity for [3H]D-AP5 (a radiolabelled NMDA antagonist) binding sites on rat brain membranes, and as an anticonvulsant in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Amino-5-phosphonovalerate
  • Animals
  • Anticonvulsants*
  • Aspartic Acid / analogs & derivatives*
  • Aspartic Acid / antagonists & inhibitors
  • Binding Sites
  • Brain / drug effects
  • Brain / metabolism
  • Brain / physiology*
  • Cats
  • Cell Membrane / metabolism
  • Interneurons / physiology
  • Membrane Potentials / drug effects
  • Mice
  • Motor Neurons / physiology
  • N-Methylaspartate
  • Neurons / drug effects
  • Neurons / physiology*
  • Piperazines / pharmacology*
  • Rats
  • Spinal Cord / drug effects
  • Spinal Cord / physiology*
  • Valine / analogs & derivatives*
  • Valine / metabolism

Substances

  • Anticonvulsants
  • Piperazines
  • Aspartic Acid
  • N-Methylaspartate
  • 2-Amino-5-phosphonovalerate
  • 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid
  • Valine