Antioxidants and Redox Signaling · 2010 · 11 citations · 25 references
MedicineNeurosciencePharmacologyNeurochemistryNeurodegenerationNeuropharmacologyDopaminergic PharmacologyMonoamine NeurochemistryNeurochemical PharmacologyNeurodegenerative Disease PharmacologyNeuroprotectionNeuroprotective PharmacologyCytochrome P450 PathwaysDopaminergic NeuroprotectionMonoamine Oxidase InhibitionMonoamine Oxidase InvolvementNeuroprotective AgentsNeuroprotective ResponsesOxidative Stress In NeurodegenerationParkinsonian Neuroprotection
The anti-Parkinsonian, monoamine oxidase-B inhibitor drug, rasagiline (Azilect®), is primarily metabolized by hepatic cytochrome P450 isoenzyme 1A2-mediated N-dealkylation to form its major metabolite, 1-(R)-aminoindan. The present study was undertaken to further investigate, for the first time, the possible neuroprotective effect of 1-(R)-aminoindan in two rat models of Parkinson's disease, the 6-hydroxydopamine- and lactacystin (a proteasomal inhibitor)-induced nigrostriatal degeneration. 1-(R)-aminoindan reversed behavioral asymmetry and restored striatal catecholamine levels in these two rat models and significantly protected neurons from hydrogen peroxide-induced oxidative stress. These observations indicate that 1-(R)-aminoindan may contribute to the overall neuroprotective activity of its parental compound, rasagiline.
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Deprenyl is metabolized to methamphetamine and amphetamine in man.
J. D. Elsworth, K. Blau, M. Sandler et al. · British Journal of Clinical Pharmacology · 1978 · 286 citations · Full text
Medicine, Pharmacology, Psychiatry +10
Proteasome inhibition causes nigral degeneration with inclusion bodies in rats
Kevin St. P. McNaught, Lars M. Bj rklund, Roger Belizaire et al. · Neuroreport · 2002 · 272 citations