Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively.
体外研究
Rasagiline (0.25 nM; 96 hours) significantly increases the proliferation rates of SH-SY5Y and 1242-MG upon Dexamethasone (10 µM) treatment.
Cell Viability Assay
Cell Line:
Neuroblastoma SH-SY5Y, and glioblastoma 1242-MG
Concentration:
0.25 nM
Incubation Time:
96 hours
Result:
Caused ~60% increase in the cell proliferation rate for SH-SY5Y cells treated with Dexamethasone.
Caused ~35% increase in cell proliferation rate for 1242-MG cells treated with Dexamethasone.
体内研究
Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Motor behavioural tests show improvements in motor deficits associated with 2.5 mg/kg Rasagiline therapy.
Animal Model:
(PLP)-α-synuclein transgenic mice over 6 months of age
Dosage:
Low-(0.8 mg/kg b.w.) and high dose (2.5 mg/kg b. w.)
Administration:
Administered subcutaneously every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment).
Result:
Low dose treatment did not show protective efficacy in striatum with number of neurons similar to placebo treated MSA mice. High dose was associated with about 15% rescue of DARPP-32 immunoreactive striatal neurons.
Low dose treatment had no effect on nigral neuronal loss, but high dose completely protected nigral neurons with numbers comparable to healthy controls.
分子式
C12H13N.CH4O3S
分子量
267.34
CAS号
161735-79-1
中文名称
雷沙吉兰甲磺酸;甲磺酸雷沙吉兰
运输条件
Room temperature in continental US; may vary elsewhere.