title: Imipramine inhibits soluble enkephalin-degrading aminopeptidase activity in vitro.
abstract: Considerable evidence has appeared recently connecting the mechanism of action of some antidepressant drugs with the inhibition of the enzymes responsible for enkephalin degradation. Imipramine in vitro inhibits the enkephalin-degrading aminopeptidase MII and interacts with the enzyme in a mixed competitive-noncompetitive manner. The present work shows that imipramine in vitro also inhibits reversibly soluble enkephalin-degrading aminopeptidase activity in rat brain. Kinetic analysis showed that this enzyme has two different binding sites for the drug, and that imipramine interacts with the enzyme in a mixed noncompetitive-acompetitive way.
authors.affiliation: Department of Physiology, School of Pharmacy, University of the Basque Country, Vitoria, Spain.
authors.forename: M
authors.initials: M
authors.lastname: Gallego
authors.forename: L
authors.initials: L
authors.lastname: Casis
authors.forename: O
authors.initials: O
authors.lastname: Casis
mesh_terms: D000626:Aminopeptidases / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004745:Enkephalins / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology; D007099:Imipramine / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D000929:Antidepressive Agents, Tricyclic; D004745:Enkephalins; D004791:Enzyme Inhibitors; D000626:Aminopeptidases; D007099:Imipramine