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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 .
4129 109731 Ensembl ENSG00000069535 ENSMUSG00000040147 UniProt P27338 Q8BW75 RefSeq (mRNA) NM_000898 NM_172778 RefSeq (protein) NP_000889 NP_766366 Location (UCSC) Chr X: 43.77 – 43.88 Mb Chr X: 16.58 – 16.68 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Monoamine oxidase B (MAO-B) is an enzyme that in humans is encoded by the MAOB gene. The protein encoded by this gene belongs ...
It is selective for inhibition of MAO-B over MAO-A, but can also inhibit MAO-A at high doses or concentrations. [1] [2] MAO-B is involved in the metabolism of the monoamine neurotransmitter dopamine in the body and brain. [1] [2] By inhibiting MAO-B, rasagiline is thought to increase dopamine levels.
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]
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 ]
[3] 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]