Inhibition of rat brain monoamine oxidase type A by 2- aminotetralin and tetrahydroisoquinoline analogues of dopamine
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Thein vitro inhibition of rat brain monoamine oxidase type A (Mao-a) by various dopamine analogues is reported and compared to some established inhibitors of the enzyme. The estimated ic50's were found to be in the range 10−5–10−3 mol/1. This makes these compounds more than 10 000 times less potent than the selectiveMao-a inhibitor harmaline and more than 10 times less potent than the selectiveMao-b inhibitors pargyline and deprenyl. When the brain concentrations that are reached after peripheral administration of these drugs are taken into account it is unlikely that inhibition ofMao is relevant to their effects as has been suggested. Also the endogenous brain concentrations of some tetrahydroisoquinolines are probably too low to produce an inhibition of the enzyme.
KeywordsPublic Health Internal Medicine Dopamine Monoamine Monoamine Oxidase
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