Receptor Binding Profile of Quinupramine, a New Tricyclic Antidepressant

Abstract

The receptor binding profile, composed of the K_i-values measured in eight different receptor binding models using rat brain membranes, is reported for the new tricyclic antidepressant quinupramine, 10, 11-dihydro-5-(3-quinuclidinyl)-5H-dibenz[b, f]azepine, and three reference compounds with a tertiaryamine side chain. Quinupramine was found to possess high affinity for muscarinic cholinergic and histamine H₁ receptor binding sites in rat brain, whereas its affinity for imipramine binding sites was only one seventieth that of imipramine. Receptor binding profiles of the reference compounds were almost similar to that of quinupramine, except in the case of imipramine binding sites.