CLORGYLINE HYDROCHLORIDE

Description

Clorgyline is a potent monoamine oxidase (MAO) inhibitor that preferentially targets MAO-A over MAO-B (K_is = 0.054 and 58 μM, respectively). This inhibition is irreversible. Clorgyline is without effect on serotonin receptors, but it does inhibit the sigma receptor σ₁ on Jurkat human T lymphocyte cells (IC₅₀ = 31 nM). As MAO-A preferentially oxidizes serotonin, selective MAO-A inhibitors have applications in ameliorating depression and anxiety.

Uses

Antidepressant;Monoamine oxidase A inhibitor

Uses

N-Methyl-N-propargyl-3-(2,4-dichlorophenoxy)propylamine hydrochloride has been used as a monoamine oxidase A (MAO-A) inhibitor:

• in MAO-A biochemical assay
• to study its effects on the transit of serotonin (5-HT) in the human placenta explants
• to study its effects on human prostate cancer cells

Biochem/physiol Actions

MAO-A inhibitor.

References

[1]. abdelhafez om, amin km, ali hi, et al. synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase a inhibitors. j med chem. 2012 dec 13;55(23):10424-36.
[2]. mazouz f, gueddari s, burstein c, et al. 5-[4-(benzyloxy)phenyl]-1,3,4-oxadiazol-2(3h)-one derivatives and related analogues: new reversible, highly potent, and selective monamine oxidase type b inhibitors. j med chem. 1993 apr 30;36(9):1157-67.
[3]. garcia-miralles m, ooi j, ferrari bardile c, et al. treatment with the mao-a inhibitor clorgyline elevates monoamine neurotransmitter levels and improves affective phenotypes in a mouse model of huntington disease. exp neurol. 2016 apr;278:4-10.