Effect of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-1-propanone fumarate, a novel acetylcholinesterase inhibitor, on spatial cognitive impairment induced by chronic cerebral hypoperfusion in rats

Neurosci Lett. 2002 Oct 4;331(1):33-6. doi: 10.1016/s0304-3940(02)00830-3.

Abstract

It is of interest whether the acetylcholinesterase inhibitor, 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-1-propanone fumarate (TAK-147), can improve cognitive impairment caused by chronic cerebral ischemia in rats. Two weeks after four-vessel occlusion, apparent impairments of spatial retrieval memory were observed in the Morris water maze. Both TAK-147 at doses of 0.1, 0.3 and 1.0 mg/kg and donepezil at doses of 0.3 and 1.0 mg/kg significantly ameliorated ischemia-induced memory deficits dose-dependently, but tacrine had no appreciable effect. Furthermore, we demonstrate that the intensity of staining by 2,3,5-triphenyltetrazolium in the hippocampal and cortical slices was significantly decreased by ischemia (10 min anoxia/aglycemia), and that it was also significantly restored by treatment with TAK-147 and donepezil.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzazepines / pharmacology*
  • Brain / drug effects
  • Brain Ischemia / drug therapy*
  • Brain Ischemia / metabolism
  • Brain Ischemia / physiopathology
  • Cholinesterase Inhibitors / pharmacology*
  • Coloring Agents
  • Donepezil
  • Dose-Response Relationship, Drug
  • Indans / pharmacology
  • Male
  • Maze Learning / drug effects*
  • Neuroprotective Agents / pharmacology
  • Organ Culture Techniques
  • Piperidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Tacrine / pharmacology
  • Tetrazolium Salts

Substances

  • Benzazepines
  • Cholinesterase Inhibitors
  • Coloring Agents
  • Indans
  • Neuroprotective Agents
  • Piperidines
  • Tetrazolium Salts
  • Tacrine
  • triphenyltetrazolium
  • TAK 147
  • Donepezil