Desmethylselegiline
Desmethylselegiline[edit | edit source]
Desmethylselegiline, also known as N-desmethylselegiline, is a chemical compound that is a metabolite of the drug selegiline. It is primarily known for its role in the pharmacological effects of selegiline, which is used in the treatment of Parkinson's disease and major depressive disorder.
Chemical Properties[edit | edit source]
Desmethylselegiline is a derivative of selegiline, formed by the demethylation of the N-methyl group. Its chemical structure is characterized by the presence of a propargylamine moiety, which is crucial for its biological activity. The compound is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B), an enzyme that breaks down dopamine in the brain.
Pharmacology[edit | edit source]
Desmethylselegiline retains the MAO-B inhibitory activity of its parent compound, selegiline. By inhibiting MAO-B, desmethylselegiline increases the levels of dopamine in the brain, which is beneficial in the management of Parkinson's disease. This action helps alleviate symptoms such as tremors, stiffness, and bradykinesia.
In addition to its effects on dopamine, desmethylselegiline may also influence other neurotransmitter systems, contributing to its antidepressant properties. The compound's ability to modulate the dopaminergic system is thought to underlie its potential therapeutic effects in mood disorders.
Clinical Significance[edit | edit source]
Desmethylselegiline is not used as a standalone medication but is an important active metabolite of selegiline. Understanding its role helps in optimizing the therapeutic use of selegiline, particularly in adjusting dosages and predicting patient responses. The presence of desmethylselegiline in the body can also be a marker for compliance in patients prescribed selegiline.
Research and Development[edit | edit source]
Research into desmethylselegiline has focused on its pharmacokinetics and pharmacodynamics. Studies have explored its potential neuroprotective effects, which may extend beyond the treatment of Parkinson's disease. The compound's ability to inhibit MAO-B without affecting MAO-A at therapeutic doses is of particular interest, as it reduces the risk of hypertensive crises associated with non-selective MAO inhibitors.
Related Compounds[edit | edit source]
Desmethylselegiline is related to other MAO-B inhibitors, such as rasagiline and safinamide. These compounds share similar mechanisms of action but differ in their pharmacokinetic profiles and clinical applications.
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