Bis(7)-tacrine, a novel acetylcholinesterase inhibitor, reverses AF64A-induced deficits in navigational memory in rats

Neurosci Lett. 2000 Mar 24;282(3):165-8. doi: 10.1016/s0304-3940(00)00905-8.

Abstract

The novel dimer bis(7)-tacrine (1,7-N-Heptylene-bis-9,9'-amino-1,2,3, 4-tetrahydroacridine), which exhibits higher potency, selectivity and oral activity on acetylcholinesterase inhibition in vivo than tacrine, was evaluated for its ability to reverse AF64A-induced spatial memory impairment in rats using the Morris water maze. The intracerebroventricular injection of AF64A (3 nmol/side) resulted in a substantial increase in the escape latency to find the platform (F(1,7)=30.2, P<0.01). The observed impairment of spatial memory was paralleled by a 47% decrease in choline acetyltransferase activity in the hippocampus. Oral administration of bis(7)-tacrine (0.22-0.89 micromol/kg) dose-dependently reversed the AF64A-induced latency delay to the level of the saline control group (F(4,28)=7.45, P<0. 05). The present study provides additional evidence of bis(7)-tacrine as an ideal candidate for the palliative treatment of Alzheimer's disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aziridines* / administration & dosage
  • Choline / administration & dosage
  • Choline / analogs & derivatives*
  • Cholinesterase Inhibitors / pharmacology*
  • Escape Reaction / drug effects
  • Injections, Intraventricular
  • Male
  • Maze Learning / drug effects
  • Memory / drug effects*
  • Rats
  • Rats, Sprague-Dawley
  • Reaction Time / drug effects
  • Tacrine / analogs & derivatives*
  • Tacrine / pharmacology
  • Toxins, Biological* / administration & dosage

Substances

  • 1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydroacridine
  • Aziridines
  • Cholinesterase Inhibitors
  • Toxins, Biological
  • Tacrine
  • ethylcholine aziridinium
  • Choline