Rasagiline mesylate 是一种高效的，不可逆的选择性线粒体单胺氧化酶 (MAO) 抑制剂，抑制大鼠脑 MAO B 和 MAO A 的IC50分别为 4.43 nM 和 412 nM。

Rasagiline Mesylate is a novel MAO-B inhibitor, which can treat 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. [1] 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. [2] 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. [3] 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. [4]

Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. [1] 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. [5]

161735-79-1

C13H17NO3S

267.34

甲磺酸雷沙吉兰;AGN1135;Azilect;TVP1012

DMSO:198.2 mM
H2O:93.51mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years