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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 ]
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. [4] [5]
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 dopamine , norepinephrine , and serotonin .
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.
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.
[19] [13] [49] [47] [50] [51] Brain MAO-B levels recover slowly upon discontinuation of selegiline, with a half-time of brain MAO-B synthesis and recovery of approximately 40 days in humans. [19] [48] Selegiline inhibits MAO-B by 50% at a very low concentration of 26 pg/mL in vivo, indicating that it is a very potent MAO-B inhibitor. [36]
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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.