2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity

Bioorg Med Chem. 1997 Dec;5(12):2129-32. doi: 10.1016/s0968-0896(97)00156-9.

Abstract

2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo.

MeSH terms

  • Animals
  • Avoidance Learning / drug effects
  • Binding Sites / drug effects
  • Cyclic N-Oxides / chemical synthesis
  • Cyclic N-Oxides / pharmacology*
  • Dizocilpine Maleate / pharmacology
  • Excitatory Amino Acid Antagonists / pharmacology
  • Glycine / antagonists & inhibitors*
  • Glycine / drug effects
  • Kynurenic Acid / analogs & derivatives
  • Kynurenic Acid / pharmacology
  • Mice
  • Motor Activity / drug effects
  • N-Methylaspartate
  • Neuroprotective Agents / pharmacology*
  • Pyrazines / chemical synthesis
  • Pyrazines / pharmacology*
  • Rats
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Seizures / prevention & control
  • Stereotyped Behavior / drug effects
  • Strychnine / pharmacology

Substances

  • 2,3-dihydro-6,7-dichloropyrido(2,3-b)pyrazine-8-oxide
  • Cyclic N-Oxides
  • Excitatory Amino Acid Antagonists
  • Neuroprotective Agents
  • Pyrazines
  • Receptors, N-Methyl-D-Aspartate
  • N-Methylaspartate
  • Dizocilpine Maleate
  • Kynurenic Acid
  • Strychnine
  • 7-chlorokynurenic acid
  • Glycine