Catalog No.S2102 Synonyms: TVP-1012
Molecular Weight(MW): 267.34
Rasagiline Mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
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|Description||Rasagiline Mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.|
Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro.  Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells.  Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death.  Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase. 
|In vivo||Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively.  Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse. |
-  Youdim MB, et al. Br J Pharmacol, 2001, 132(2), 500-506.
-  Maruyama W, et al. J Neurochem, 2001, 78(4), 727-735.
-  Youdim MB, et al. Ann N Y Acad Sci, 2001, 939, 450-458.
|In vitro||DMSO||53 mg/mL (198.24 mM)|
|Water||53 mg/mL (198.24 mM)|
|Ethanol||53 mg/mL (198.24 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01879241||Completed||Drug: Rasagiline|Drug: Placebo||Amyotrophic Lateral Sclerosis||University of Ulm||June 2013||Phase 2|
|NCT01652313||Completed||Drug: Rasagiline||Parkinson''s Disease||H. Lundbeck A/S||May 2012||Phase 1|
|NCT01736891||Completed||Drug: Rasagiline|Drug: Placebo||Parkinson´s Disease||Chongqing Fortune Pharmaceutical Co. Ltd.|Beijing Bionovo Medicine Development Co. Ltd.||November 2011||Phase 3|
|NCT01178047||Terminated||Drug: Rasagiline||Parkinson''s Disease||University of Zurich|H. Lundbeck A/S||September 2011||Phase 4|
|NCT01055379||Completed||Drug: Rasagiline|Drug: Placebo||Depressive Symptoms|Parkinson''s Disease||Lundbeck Italia S.p.A.|Teva Pharmaceutical Industries||March 2010||Phase 4|
|NCT00203164||Completed||Drug: rasagiline mesylate||Parkinson''s Disease||Teva Pharmaceutical Industries||May 2002||Phase 3|
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