The AMPA receptor/Na(+) channel blocker BIIR 561 CL is protective in a model of global cerebral ischaemia

Eur J Pharmacol. 2001 Jun 15;421(3):165-70. doi: 10.1016/s0014-2999(01)01031-7.

Abstract

In this study, we investigated whether the novel neuroprotective compound dimethyl-[2-[2-(3-phenyl-[1,2,4]oxadiazol-5-yl)-phenoxy]-ethyl]-amine hydrochloride, BIIR 561 CL, a combined non-competitive antagonist of AMPA receptors and blocker of voltage-gated Na+ channels, is protective in a rat model of severe global ischaemia. BIIR 561 CL administered immediately after 10 min of ischaemia (occlusion of both carotid arteries plus reduction of arterial blood pressure to 38-40 mm Hg) significantly reduced hippocampal damage at 4 x 26.8 mg/kg (subcutaneous injections). The competitive AMPA receptor antagonist 2,3-dihydro-6-nitro-7-sulfamoyl-benz(F)quinoxaline, NBQX, was used as a reference compound and was protective at 3x30 mg/kg (intraperitoneal and/or subcutaneous administration). BIIR 561 CL significantly reduced the ischaemia-induced premature mortality from 33.6% in the controls to 14.3%, whereas NBQX treatment had no statistically significant effect.Thus, BIIR 561 CL could be shown to reduce hippocampal damage and premature mortality in a model of severe global ischaemia. A compound with these properties might be an interesting candidate for the treatment of disorders related to global cerebral ischaemia in man.

MeSH terms

  • Animals
  • Brain Ischemia / mortality
  • Brain Ischemia / prevention & control*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Hippocampus / drug effects
  • Hippocampus / pathology
  • Male
  • Neuroprotective Agents / pharmacology*
  • Oxadiazoles / pharmacology*
  • Quinoxalines / pharmacology
  • Rats
  • Rats, Wistar
  • Receptors, AMPA / antagonists & inhibitors*
  • Sodium Channel Blockers*
  • Survival Rate

Substances

  • Neuroprotective Agents
  • Oxadiazoles
  • Quinoxalines
  • Receptors, AMPA
  • Sodium Channel Blockers
  • 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline
  • irampanel