Glycine derivatives of imidazolones as potential ligands of glycine binding site of NMDA receptors. Part 1

Acta Pol Pharm. 1998 Sep-Oct;55(5):381-8.

Abstract

The series of glycine derivatives of diphenyl or (un)substituted arylidene imidazolones was designed and obtained as potential ligands of the glycine binding site of NMDA receptors. The compounds were evaluated in vitro for their affinity to the glycine binding site of NMDA receptors using as radioligand [3H]-L-689,560. Their anticonvulsant activity was estimated in vivo in maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scMet) tests. To explain the structure, pharmacological activity results Multiple Linear Regression Analysis was used.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology
  • Convulsants / pharmacology
  • Electroshock
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology*
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • Ligands
  • Male
  • Mice
  • Pentylenetetrazole / antagonists & inhibitors
  • Rats
  • Receptors, Glycine / drug effects*
  • Receptors, N-Methyl-D-Aspartate / drug effects*
  • Seizures / chemically induced
  • Seizures / prevention & control

Substances

  • Anticonvulsants
  • Convulsants
  • Imidazoles
  • Ligands
  • Receptors, Glycine
  • Receptors, N-Methyl-D-Aspartate
  • Glycine
  • Pentylenetetrazole