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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 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 .
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.
2-NAP is a potent monoamine oxidase inhibitor (MAOI), specifically of monoamine oxidase A (MAO-A) (IC 50 Tooltip half-maximal effective concentration = 420 nM). [8] [3] 1-NAP is an MAOI as well, also of MAO-A (IC 50 = 5,630 nM), but was about 13-fold less potent than 2-NAP. [3] Neither 2-NAP or 1-NAP inhibited monoamine oxidase B (MAO-B) (IC 50 ...
[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]
It is a dual or non-selective irreversible monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) inhibitor, with preference for inhibition of MAO-B over MAO-A. [3] [4] It is less selective for MAO-B inhibition than AGN-1135 (racemic rasagiline) or rasagiline. [3]
Reversible inhibitors of MAO-A (16 P) Pages in category "Monoamine oxidase inhibitors" The following 118 pages are in this category, out of 118 total.
In vertebrates, MAO plays an important role in regulating the intracellular levels of amines via their oxidation; these include various neurotransmitters, neurotoxins and trace amines. [3] In lower eukaryotes such as aspergillus and in bacteria the main role of amine oxidases is to provide a source of ammonium. [ 4 ]