Mofegiline

Mofegiline

Mofegiline (MDL 72,974A) is a drug that acts as a selective inhibitor of the enzyme monoamine oxidase B (MAO-B). This enzyme is involved in the breakdown of neurotransmitters such as dopamine, making mofegiline of interest in the treatment of neurological conditions such as Parkinson's disease. By inhibiting MAO-B, mofegiline increases the availability of dopamine in the brain, which can help to alleviate the symptoms of Parkinson's disease, a condition characterized by reduced dopamine levels.

Pharmacology

Mofegiline's mechanism of action involves the selective inhibition of monoamine oxidase B, an enzyme that degrades dopamine, a critical neurotransmitter in the regulation of movement, mood, and reward. Unlike non-selective monoamine oxidase inhibitors (MAOIs) that affect both MAO-A and MAO-B enzymes and can lead to significant side effects and dietary restrictions, mofegiline's selectivity for MAO-B allows for increased dopamine levels without the same level of risk.

Clinical Use

While mofegiline showed promise in early clinical trials for the treatment of Parkinson's disease, its development was eventually discontinued. The reasons for this are not detailed in public records but could include a range of factors from lack of efficacy in larger trials, safety concerns, or commercial decisions. Despite this, the study of mofegiline has contributed to the understanding of MAO-B's role in neurodegenerative diseases and the potential for selective inhibitors in therapeutic applications.

Research

Research on mofegiline has provided valuable insights into the pharmacological targeting of MAO-B as a strategy for increasing dopamine levels in the brain. This has implications not only for Parkinson's disease but also for other conditions characterized by reduced dopamine activity, such as certain forms of depression and neurodegenerative disorders. The development and study of mofegiline have helped pave the way for other MAO-B inhibitors that are currently in use or under investigation.

See Also

• Monoamine oxidase inhibitor
• Parkinson's disease
• Neurotransmitter
• Dopamine

‎