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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.
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 .
Brunner syndrome is caused by a monoamine oxidase A (MAOA) deficiency, which leads to an excess of monoamines in the brain, such as serotonin, dopamine, and norepinephrine (noradrenaline). In both mice and humans, a mutation was located on the eighth exon of the MAO-A gene, which created a dysfunctional MAO-A gene.
Tranylcypromine reaches its maximum concentration (t max) within 1–2 hours. [20] After a 20 mg dose, plasma concentrations reach at most 50-200 ng/mL. [20] While its half-life is only about 2 hours, its pharmacodynamic effects last several days to weeks due to irreversible inhibition of MAO. [20]
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 ...
It is most efficacious as a releaser of norepinephrine, with an EC 50 of 109 nM (DA), 41.4 nM (NE), and 5,246 nM . [ 2 ] It also functions as a weak monoamine oxidase inhibitor (MAOI) ( IC 50 Tooltip half-maximal inhibitory concentration = 130 μM for MAO-A Tooltip monoamine oxidase A and 750 μM for MAO-B Tooltip monoamine oxidase B ).
Harmine is a beta-carboline and a harmala alkaloid.It occurs in a number of different plants, most notably the Syrian rue and Banisteriopsis caapi. [3] Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a Reversible inhibitor of monoamine oxidase A (RIMA).