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The neuroprotective mechanism of 1‐( R )‐aminoindan, the major metabolite of the anti‐parkinsonian drug rasagiline
Author(s) -
BarAm Orit,
Weinreb Orly,
Amit Tamar,
Youdim Moussa B. H.
Publication year - 2010
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.2009.06542.x
Subject(s) - rasagiline , neuroprotection , pharmacology , metabolite , selegiline , levodopa , drug , parkinson's disease , monoamine oxidase b , chemistry , monoamine oxidase , medicine , biochemistry , enzyme , disease
J. Neurochem. (2010) 112 , 1131–1137. Abstract The anti‐parkinsonian drug, rasagiline [ N ‐propargyl‐1‐( R )‐aminoindan; Azilect®], is a secondary cyclic benzylamine and indane derivative, which provides irreversible, potent monoamine oxidase‐B (MAO‐B) inhibition and possesses neuroprotective and neurorestorative activities. A prospective clinical trial has shown that rasagiline confers significant symptomatic improvement and demonstrated alterations in Parkinson’s disease progression. Rasagiline is primarily metabolized by hepatic cytochrome P‐450 to form its major metabolite, 1‐( R )‐aminoindan, a non‐amphetamine, weak reversible MAO‐B inhibitor compound. Recent studies indicated the potential neuroprotective effect of 1‐( R )‐aminoindan, suggesting that it may contribute to the overall neuroprotective and antiapoptotic effects of its parent compound, rasagiline. This review article briefly highlights the molecular mechanisms underlying the neuroprotective properties of the active metabolite of rasagiline, 1‐( R )‐aminoindan, supporting the valuable potential of rasagiline for disease modification.