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Rasagiline Mesylate

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Chemical Structure| 161735-79-1 同义名 : TVP1012 mesylate;(R)-AGN1135 mesylate
CAS号 : 161735-79-1
货号 : A262921
分子式 : C13H17NO3S
纯度 : 97%
分子量 : 267.344
MDL号 : MFCD08460604
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 25 mg/mL(93.51 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Rasagiline 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. The ED(50) values for ex vivo inhibition of MAO in the brain and liver by a single dose of rasagiline are 0.1+/-0.01, 0.042+/-0.0045 mg/kg respectively for MAO-B, and 6.48+/-0.81, 2.38+/-0.35 mg/kg respectively for MAO-A. Rasagiline was 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 had similar potency in vitro[3]. Rasagiline improves motor fluctuations and Parkinson disease (PD) symptoms in levodopa-treated PD patients[4]. Rasagiline (up to 2 mg/day) has a good safety profile and a beneficial clinical effect in fluctuating patients with PD when given as an add-on to chronic levodopa therapy[5]. Moreover, Rasagiline Mesylate has a positive effect in the post-MI (myocardial infarction) period with a significant attenuation in cardiac remodelling[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01280123 Parkinson's Disease Phase 2 Completed - -
NCT01280123 - Completed - -
NCT01155466 Parkinson Disease Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.74mL

0.75mL

0.37mL

18.70mL

3.74mL

1.87mL

37.40mL

7.48mL

3.74mL
参考文献

[1]Maruyama W, Akao Y, et al. Transfection-enforced Bcl-2 overexpression and an anti-Parkinson drug, rasagiline, prevent nuclear accumulation of glyceraldehyde-3-phosphate dehydrogenase induced by an endogenous dopaminergic neurotoxin, N-methyl(R)salsolinol. J Neurochem. 2001 Aug;78(4):727-35.

[2]Youdim MB, Gross A, Finberg JP. Rasagiline [N-propargyl-1R(+)-aminoindan] , a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6.

[3]Youdim MB, Gross A, Finberg JP. Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6

[4]Parkinson Study Group. A randomized placebo-controlled trial of rasagiline in levodopa-treated patients with Parkinson disease and motor fluctuations: the PRESTO study. Arch Neurol. 2005 Feb;62(2):241-8

[5]Rabey JM, Sagi I, Huberman M, Melamed E, Korczyn A, Giladi N, Inzelberg R, Djaldetti R, Klein C, Berecz G; Rasagiline Study Group. Rasagiline mesylate, a new MAO-B inhibitor for the treatment of Parkinson's disease: a double-blind study as adjunctive therapy to levodopa. Clin Neuropharmacol. 2000 Nov-Dec;23(6):324-30

[6]Varela A, Mavroidis M, Katsimpoulas M, Sfiroera I, Kappa N, Mesa A, Kostomitsopoulos NG, Cokkinos DV. The neuroprotective agent Rasagiline mesylate attenuates cardiac remodeling after experimental myocardial infarction. ESC Heart Fail. 2017 Aug;4(3):331-340