1H-Inden-1-amine,2,3-dihydro-N-2-propyn-1-yl-, (1R)-
(R)-2,3-DIHYDRO-N-2-PROPYNYL-1H-INDEN-1-AMINE;Rasagiline -13C3;Rasagiline;(R)-N-2-Propynyl-1-indanamine;1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (1R);1-Indanamine, N-2-propynyl-, (R)-;Unii-003N66ts6t;(R)-N-(2-Propynyl)-2,3-dihydroinden-1-aMine
Rezagiline use and synthesis methods
Parkinson's disease (PD) is a common chronic nervous system degenerative disease. All ages can be disease, but mostly in the elderly. With the aging of the population, its incidence increased year by year, and the incidence of young people showed a trend, to the family and society caused a heavy burden. L-dopa is still the most effective drug for the treatment of PD, but in the use of 2 to 5 years after the emergence of efficacy and long-term side effects, such as movement fluctuations (including the phenomenon of the end of the phenomenon, the phenomenon of switching and freezing phenomenon) And dyskinesia (including biphasic dyskinesia and dystonia).
Rasagiline (Rasagiline, trade name Azilect) is a Parkinson's disease treatment drug, by Lundbeck and Teva long-term alliance with the joint development of Parkinson's disease (PD) treatment drugs, is a new and effective second generation Selective monoamine oxidase B (MAO-B) inhibitors. The drug was first listed in Israel in January 2005 and subsequently approved by the European Union in February 2005 for the first time in June 2005 in the EU countries and has been approved by the FDA.
Raisagiline is an irreversible B-type monoamine oxidase (MAO-B) selective inhibitor that inhibits dopamine degradation and increases dopamine accumulation; while reducing synaptic membrane pre-dopamine uptake, promoting dopamine release, improving PD patients Clinical symptoms. It is in the prevention of tremor paralysis caused by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (1 -methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP) Bisi Li Gelan effective 5 times. The main metabolite of losagiline is 1- (R) -aminoindane without the addiction of amphetamines. In addition to inhibiting monoamine oxidase B, rasagiline can also prevent the opening of mitochondrial filtration pore, reduce the release of cytochrome C, alter the anti-apoptotic gene and protein, inhibit the transcription of glyceraldehyde-3-phosphate dehydrogenase, Nutritional factors. In clinical studies, rasagiline monotherapy is moderately effective and is effective in monotherapy or adjuvant treatment with levodopa, early and late PD drugs. Studies have confirmed that early use of rasagiline has a good effect on the treatment of tremor paralysis and may have delayed the role of the disease process and is now widely used clinically.