The putative cognitive enhancer KA-672.HCl is an uncompetitive voltage-dependent NMDA receptor antagonist

Neuroreport. 1998 Dec 21;9(18):4193-7. doi: 10.1097/00001756-199812210-00035.

Abstract

KA-672.HCl (KA-672) is a new substance demonstrating anti-dementia properties. It shows modulatory effects on several neurotransmitter systems known to be affected in patients with Alzheimer's disease. In this study the action of KA-672 on the NMDA receptors was examined by applying patch clamp techniques to acutely isolated hippocampal neurons. KA-672 antagonizes NMDA responses in a voltage-dependent manner. At a holding potential of -90 mV the IC50 value for the blocking action of KA-672 was 20+/-7 microM. This action of KA-672 is independent on the concentration either of agonist or coagonist of NMDA receptor. Ketamine, which interacts with the PCP center, does not occlude the action of KA-672. Evidently, KA-672.HCl is a weak NMDA receptor-operated channel blocker. This property may account for its pharmacological profile.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzopyrans / pharmacology*
  • Cognition / drug effects
  • Dose-Response Relationship, Drug
  • Electrophysiology
  • Excitatory Amino Acid Antagonists / pharmacology
  • Hippocampus / cytology
  • Hippocampus / physiology
  • Ketamine / pharmacology
  • N-Methylaspartate / antagonists & inhibitors
  • N-Methylaspartate / pharmacology
  • Neurons / drug effects
  • Neurons / physiology
  • Patch-Clamp Techniques
  • Piperazines / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Receptors, N-Methyl-D-Aspartate / physiology

Substances

  • Benzopyrans
  • Excitatory Amino Acid Antagonists
  • Piperazines
  • Receptors, N-Methyl-D-Aspartate
  • N-Methylaspartate
  • Ketamine
  • Ensaculin