Dependence of pharmacological activity of new NMDA agonists and antagonists on their chemical structure

Abstract

A group of imidazole derivatives was tested for their agonistic and antagonistic activity with respect to NMDA receptors in pyramidal neurons of the rat hippocampus. The data from the experiments using intracerebroventricular injections of the tested agents were compared with those carried out on isolated cells using a patch-clamp technique in the whole-cell configuration. It has been shown that the presence of lipophilic groups in the molecules of the above derivatives determines their ability to be NMDA antagonists.