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Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants , especially for treatment-resistant depression and atypical depression . [ 1 ]
Monoamine oxidases (MAO) (EC 1.4.3.4) are a family of enzymes that catalyze the oxidation of monoamines, employing oxygen to clip off their amine group. [ 1 ] [ 2 ] They are found bound to the outer membrane of mitochondria in most cell types of the body.
A few endogenous MAEs have been identified, including the trace amines β-phenylethylamine (PEA), tyramine, and tryptamine. [1] [11] At a concentration of 16 μM (1.6 × 10 −5 M), β-phenylethylamine has been shown to act as a MAE for norepinephrine (2.6-fold increase), dopamine (1.3-fold increase), and serotonin (2.3-fold increase) in the rat brainstem in vitro.
Monoamine oxidase A, also known as MAO-A, is an enzyme (E.C. 1.4.3.4) that in humans is encoded by the MAOA gene. [ 5 ] [ 6 ] This gene is one of two neighboring gene family members that encode mitochondrial enzymes which catalyze the oxidative deamination of amines , such as norepinephrine , serotonin and tyramine .
In addition to its MRA activity, 4-MTDMA is a fairly potent monoamine oxidase A (MAO-A) inhibitor, with an IC 50 Tooltip half-maximal inhibitory concentration of 2,100 nM. [ 4 ] [ 5 ] Potent monoamine oxidase inhibition by amphetamines has been associated with dangerous and sometimes fatal toxicity in humans.
Rasagiline acts as an inhibitor of the enzyme monoamine oxidase (MAO) and hence is a monoamine oxidase inhibitor (MAOI). [2] More specifically, it is a selective inhibitor of monoamine oxidase B (MAO-B). [2] The drug is thought to work by increasing levels of the monoamine neurotransmitter dopamine in the brain. [2]
Tryptolines are competitive selective inhibitors of the enzyme monoamine oxidase type A (). 5-Hydroxytryptoline and 5-methoxytryptoline (pinoline) are the most active monoamine oxidase inhibitors (MAOIs) with IC 50 s of 0.5 μM and 1.5 μM respectively.
Although it has been estimated that a single 300 mg dose of moclobemide inhibits 80% of monoamine oxidase-A (MAO-A) and 20-30% of MAO-B, [100] studies evaluating brain occupancy of MAO-A enzymes have shown dosages of 600 mg to only inhibit 74% of MAO-A enzymes [101] and dosages in the 900–1200 mg range to inhibit slightly less MAO-A than ...