title: Inhibitory potency of some isatin analogues on human monoamine oxidase A and B.
abstract: Isatin is an endogenous compound which acts as a selective inhibitor of monoamine oxidase (MAO) B. In this study a range of isatin analogues were tested for their in vitro inhibition of human MAO A and B. Most of the analogues were less potent than isatin. Hydroxylation of the aromatic ring changed the inhibitory potency in favour of MAO A, with 5-hydroxyisatin being a potent and selective MAO A inhibitor (IC50 8 microM). Isatinic acid, which is formed reversibly from isatin at alkaline pH, showed no inhibition.
authors.affiliation: Institute of Biological and Medical Chemistry, Academy of Medical Sciences, Moscow, Russia.
authors.forename: A E
authors.initials: AE
authors.lastname: Medvedev
authors.forename: B
authors.initials: B
authors.lastname: Goodwin
authors.forename: A
authors.initials: A
authors.lastname: Clow
authors.forename: J
authors.initials: J
authors.lastname: Halket
authors.forename: V
authors.initials: V
authors.lastname: Glover
authors.forename: M
authors.initials: M
authors.lastname: Sandler
mesh_terms: D001792:Blood Platelets / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006900:Hydroxylation; D007510:Isatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010920:Placenta / Q000187:drug effects
chemical_list: D008996:Monoamine Oxidase Inhibitors; D007510:Isatin; D008995:Monoamine Oxidase