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Rasagiline [N‐propargyl‐1R(+)‐aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B
Data indicate that this inhibitor like selegiline may be a useful agent in the treatment of Parkinson's disease in either symptomatic or L‐DOPA adjunct therapy, but lack of amphetamine‐like metabolites could present a therapeutic advantage for rasagiline.
TV3326, a novel neuroprotective drug with cholinesterase and monoamine oxidase inhibitory activities for the treatment of Alzheimer's disease.
TV3326 and TV3279 protect against ischemia-induced cytotoxicity in PC12 cells and reduce the oedema, deficits in motor function and memory after closed head injury in mice and shows selectivity for brain MAO, even after 2 months of daily administration, with little or no effect on the enzyme in the intestinal tract and liver.
Apomorphine enantiomers protect cultured pheochromocytoma (PC12) cells from oxidative stress induced by H2O2 and 6‐hydroxydopamine
It is shown that 1–10 μM of apomorphine protects rat pheochromocytoma (PC12) cells from the toxic effects of H2O2 and the neurotoxin 6‐hydroxydopamine and one may assume that apomorphines can exert a neuroprotective activity via its potent antioxidant properties.
Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects
- O. Cohen‐Barak, Jacqueline A L Wildeman, O. Spiegelstein
- Biology, MedicineJournal of clinical pharmacology
- 12 January 2015
TV‐1380 is found to be safe and well tolerated with a long half‐life and showed a dose‐proportional increase in systemic exposure and offers a safe once‐weekly therapy to increase cocaine hydrolysis.
Limited potentiation of blood pressure response to oral tyramine by brain-selective monoamine oxidase A-B inhibitor, TV-3326 in conscious rabbits 1 1 Supported by Teva Pharmaceuticals Ltd…
A possible new role for fish retinal serotonin-N-acetyltransferase-1 (AANAT1): Dopamine metabolism
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
The observed SAR offers insight into the requirements of the active sites on these enzymes, and is likely that these compounds will be metabolized to the corresponding phenols, with inhibitory activities against AChE and/or MAO-A or -B, different from those of the parent carbamates.
A novel cholinesterase and brain-selective monoamine oxidase inhibitor for the treatment of dementia comorbid with depression and Parkinson's disease
Apomorphine enantiomers protect cultured pheochromocytoma (PC12) cells from oxidative stress induced by H2O2 and 6‐Hydroxydopamine
It is shown that 1–10 µM of apomorphine protects rat pheochromocytoma (PC12) cells from the toxic effects of H2O2 (0.6 mM) and the neurotoxin 6‐hydroxydopamine (150 µM) and neither of these effects were exhibited by ascorbic acid, desferal, lisuride, or bromocriptine.
Cardiovascular responses to combined treatment with selective monoamine oxidase type B inhibitors and L‐DOPA in the rat
- J. Finberg, A. Gross, O. Bar‐Am, R. Friedman, Y. Loboda, M. Youdim
- Biology, ChemistryBritish journal of pharmacology
- 1 November 2006
Rasagiline is a new, potent and selective MAO‐B inhibitor, which does not possess the sympathomimetic effects of selegiline, and is studied for its effects on the cardiovascular system of the rat.