rasagiline

Rasagiline (AGN1135) 是不可逆的、高效的、选择性的线粒体单胺氧化酶 (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 (AGN1135) 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。

(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.

Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg kg).1It reduces cerebral edema in a mouse model of traumatic brain injury.2Rasagiline (0.1 mg kg) reduces cortical and hippocampal levels of full-length and soluble amyloid precursor protein (APP) in rats and mice. It also reduces α-synuclein-induced substantia nigral neuron loss and improves motor dysfunction in a mouse model of Parkinson's disease.3Formulations containing rasagiline have been used in the treatment of Parkinson's disease. 1.Youdim, M.B.H., Gross, A., and Finberg, J.P.Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase BBrit. J. Pharmacol.132(2)500-506(2001) 2.Youdim, M.B.H., and Weinstock, M.Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R) aminoindan-5-YL)-ethyl methyl carbamate]Cell. Mol. Neurobiol.21(6)555-573(2001) 3.Kang, S.S., Ahn, E.H., Zhang, Z., et al.α-Synuclein stimulation of monoamine oxidase-B and legumain protease mediates the pathology of Parkinson's diseaseEMBO J.37(12)e98878(2018)

Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible monoamine oxidase inhibitor.

Racemic rasagiline，也称为 AGN-1135，是一种单胺氧化酶 B 型抑制剂(MAOI)。然而，在食用富含酪胺的食物的患者中，这种药物的应用可能导致致命的高血压危象。TVP-1022是雷沙吉兰的(S)异构体，具有心脏保护剂的作用。

(S)-Rasagiline mesylate is rasagiline S-isomer, and is an agent of anti-Parkinson.

2-PAT 是一种 Rasagiline 和 Selegiline 的类似物，也是可逆的 MAO-A 抑制剂，IC50为 0.721 µM。2-PAT 是 MAO-B 的灭活剂，IC50为 14.6 µM。2-PAT 具有用于帕金森病和抑郁症研究的潜力。