Drug intelligence / Profile preview

desmethyl-selegiline

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Desmethyl-selegiline is an **active metabolite of selegiline** (L-deprenyl), the anti-Parkinson and antidepressant drug[1]. Its chemical synonyms include norselegiline and N-propargyl-L-amphetamine[1]. Like selegiline, desmethyl-selegiline is a **selective and irreversible inhibitor of monoamine oxidase B (MAO-B)**, acting as a monoamine oxidase inhibitor (MAOI)[1]. It also demonstrates **catecholaminergic activity enhancer (CAE)** effects. Desmethyl-selegiline is less potent than selegiline as a MAO-B inhibitor in vitro but maintains comparable activity in vivo[1]. Unlike selegiline, which metabolizes to levomethamphetamine and levoamphetamine, desmethyl-selegiline’s main active metabolite is levoamphetamine—a dopamine and norepinephrine releasing agent with sympathomimetic and psychostimulant properties, but desmethyl-selegiline itself does not release monoamines[1]. It shows **neuroprotective, antioxidant, and antiapoptotic activity**, which are believed to be partly independent of MAO-B inhibition and may involve inhibition of glyceraldehyde-3-phosphate dehydrogenase (GAPDH)[1]. Desmethyl-selegiline has not been developed or approved for medical use and has not been marketed; its clinical research history is limited[1][3].

Other names
desmethylselegilinenorselegilineN-propargyl-L-amphetamineL-(-)-desmethylselegiline
02

Targets

MAOB (Monoamine oxidase B)

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