page_title: Tranylcypromine
section_title: Pharmacodynamics
hierarchical_section_title: Tranylcypromine / Pharmacology / Pharmacodynamics
context_page_description: Tranylcypromine is a monoamine oxidase inhibitor; more specifically, tranylcypromine acts as nonselective and irreversible inhibitor of the enzyme monoamine oxidase. It is used as an antidepressant and anxiolytic agent in the clinical treatment of mood and anxiety disorders, respectively.
  Tranylcypromine is a propylamine formed from the cyclization of amphetamine's side chain; therefore, it is classified as a substituted amphetamine.
context_section_description: Tranylcypromine acts as a nonselective and irreversible inhibitor of monoamine oxidase. Regarding the isoforms of monoamine oxidase, it shows slight preference for the MAOB isoenzyme over MAOA. This leads to an increase in the availability of monoamines, such as serotonin, norepinephrine, and dopamine, as well as a marked increase in the availability of trace amines, such as tryptamine, octopamine, and phenethylamine. The clinical relevance of increased trace amine availability is unclear.
  It may also act as a norepinephrine reuptake inhibitor at higher therapeutic doses. Compared to amphetamine, tranylcypromine shows low potency as a dopamine releasing agent, with even weaker potency for norepinephrine and serotonin release.
  Tranylcypromine has also been shown to inhibit the histone demethylase, BHC110/LSD1. Tranylcypromine inhibits this enzyme with an IC50 < 2 μM, thus acting as a small molecule inhibitor of histone demethylation with an effect to derepress the transcriptional activity of BHC110/LSD1 target genes. The clinical relevance of this effect is unknown.
  Tranylcypromine has been found to inhibit CYP46A1 at nanomolar concentrations. The clinical relevance of this effect is unknown.
caption: Mechanism of tranylcypromine inhibition of MAO.[17]
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