Monoamine oxidase inhibition by moclobemide and 2-amino-ethyl carboxamide derivatives: mode of action and kinetic characteristics.
The selective, reversible inhibitors of monoamine oxidase (MAO) moclobemide and Ro 41-1049 (selective for MAO-A), as well as of Ro 16-6491 and Ro 19-6327 (selective for MAO-B) inhibited the enzyme with an initial competitive phase, followed by a time-dependent inhibition of MAO. Ro 41-1049, Ro 16-6491 and Ro 19-6327, being activated by MAO into reversible adducts, fit into the classification as mechanism-based inhibitors. Conversely, since no product formation was observed after incubation of tissue homogenates with moclobemide, this drug probably belongs to the class of the "slow-binding" MAO inhibitors.
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Pharmaceutical Research Department, F. Hoffmann-La Roche Ltd, Basel, Switzerland.
Muggli-Maniglio
D
D
Lang
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Imhof
R
R
Da Prada
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M
D000818:Animals; D001549:Benzamides / Q000378:metabolism / Q000494:pharmacology*; D001792:Blood Platelets / Q000201:enzymology; D001921:Brain / Q000201:enzymology; D002462:Cell Membrane / Q000201:enzymology / Q000378:metabolism; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D020912:Moclobemide; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors; D010848:Picolinic Acids / Q000378:metabolism / Q000494:pharmacology; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D051381:Rats; D013844:Thiazoles / Q000378:metabolism / Q000494:pharmacology*
D001549:Benzamides; D008996:Monoamine Oxidase Inhibitors; D010848:Picolinic Acids; D013844:Thiazoles; C063456:Ro 41-1049; C059303:lazabemide; C051040:Ro 16-6491; D008995:Monoamine Oxidase; D020912:Moclobemide