Synthesis and anticonvulsant properties of tetrahydroisoquinoline derivatives

Farmaco. 2004 Jan;59(1):7-12. doi: 10.1016/j.farmac.2003.10.003.

Abstract

As a follow up of our previous structure-activity relationship and molecular modeling studies, we synthesized a novel series of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as potential non-competitive AMPA receptor antagonists. When tested for their ability to prevent sound-induced seizures in DBA/2 mice, some of these novel compounds showed high anticonvulsant potency.

Publication types

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

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology*
  • Benzodiazepines / pharmacology
  • Benzodiazepinones / pharmacology
  • Drug Evaluation, Preclinical
  • Excitatory Amino Acid Antagonists / pharmacology
  • Female
  • Male
  • Mice
  • Mice, Inbred DBA
  • Models, Molecular
  • Molecular Structure
  • Receptors, AMPA / antagonists & inhibitors
  • Seizures / prevention & control*
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines / chemical synthesis*
  • Tetrahydroisoquinolines / pharmacology*

Substances

  • Anticonvulsants
  • Benzodiazepinones
  • CFM 2
  • Excitatory Amino Acid Antagonists
  • Receptors, AMPA
  • Tetrahydroisoquinolines
  • GYKI 52466
  • Benzodiazepines
  • talampanel