p-Methoxyamphetamine, a potent reversible inhibitor of type-A monoamine oxidase in vitro and in vivo.
p-Methoxyamphetamine is over 20 times as potent as (+)-amphetamine as an inhibitor of 5-HT oxidation by monoamine oxidase in mouse brain in vitro, with a Ki value of 0.22 microM. It is highly selective towards A-type monoamine oxidase and possesses only weak activity against the B-type enzyme (Ki value about ... 500 microM with benzylamine as substrate and solubilized rat liver mitochondria as enzyme source). It is 10 times more active than (+)-amphetamine in protecting mouse brain monoamine oxidase from inhibition by phenelzine in vivo. o-Methoxy- and m-methoxyamphetamines inhibit monoamine oxidase both in vitro and in vivo with potencies comparable with, or less than that of (+)-amphetamine.
Mesh Terms:
Amphetamine, Amphetamines, Animals, Brain, Clorgyline, Dose-Response Relationship, Drug, In Vitro Techniques, Kinetics, Male, Mice, Monoamine Oxidase Inhibitors, Phenelzine, Rats, Serotonin, Structure-Activity Relationship, Substrate Specificity
Amphetamine, Amphetamines, Animals, Brain, Clorgyline, Dose-Response Relationship, Drug, In Vitro Techniques, Kinetics, Male, Mice, Monoamine Oxidase Inhibitors, Phenelzine, Rats, Serotonin, Structure-Activity Relationship, Substrate Specificity
J. Pharm. Pharmacol.
Date: Apr. 01, 1980
PubMed ID: 6103055
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