title: Relationship between imidazoline(2) sites and monoamine oxidase.
abstract: I(2) site-selective compounds are known to interact with and inhibit monoamine oxidase (MAO), but it remains unclear as to whether this interaction occurs through an allosteric or competitive interaction. This study used the new selective, irreversible I(2) ligand BU99006, to clarify the relationship between MAO and the I(2) binding sites (I(2)-BS). Results demonstrate that irreversible binding of BU99006 to rat brain membranes does not inhibit the enzyme or interfere with its interaction with other imidazoline enzyme inhibitors. This finding suggests that the I(2) sites that react with BU99006 are not those implicated in MAO inhibition and points to the existence of at least two distinct I(2) binding proteins.
authors.affiliation: Psychopharmacology Unit, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, UK.
authors.forename: L M
authors.initials: LM
authors.lastname: Paterson
authors.forename: R J
authors.initials: RJ
authors.lastname: Tyacke
authors.forename: D J
authors.initials: DJ
authors.lastname: Nutt
authors.forename: A L
authors.initials: AL
authors.lastname: Hudson
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000378:metabolism* / Q000494:pharmacology; D001921:Brain / Q000166:cytology / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D003010:Clorgyline / Q000494:pharmacology; D007093:Imidazoles / Q000378:metabolism* / Q000494:pharmacology; D054755:Imidazoline Receptors; D008024:Ligands; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011955:Receptors, Drug / Q000378:metabolism*; D012642:Selegiline / Q000494:pharmacology
chemical_list: C105826:BU 224; C468012:BU 99006; D001572:Benzofurans; D007093:Imidazoles; D054755:Imidazoline Receptors; D008024:Ligands; D008996:Monoamine Oxidase Inhibitors; D011955:Receptors, Drug; D012642:Selegiline; D008995:Monoamine Oxidase; D003010:Clorgyline