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Merck
CN

SML0124

甲磺酸雷沙吉兰 甲磺酸酯

≥98% (HPLC), MAO B inhibitor, powder

别名:

(R)-N-2-丙炔基-1-氢化茚胺甲磺酸盐 甲磺酸酯, TVP-1012, 马来酸雷沙吉兰 甲磺酸酯

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关于此项目

经验公式(希尔记法):
C12H13N · CH4O3S
化学文摘社编号:
分子量:
267.34
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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产品名称

甲磺酸雷沙吉兰 甲磺酸酯, ≥98% (HPLC)

SMILES string

CS(O)(=O)=O.C#CCN[C@@H]1CCc2ccccc12

InChI

1S/C12H13N.CH4O3S/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12;1-5(2,3)4/h1,3-6,12-13H,7-9H2;1H3,(H,2,3,4)/t12-;/m1./s1

InChI key

JDBJJCWRXSVHOQ-UTONKHPSSA-N

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +15 to +28°, c = 0.6 mg/mL in H2O

storage condition

desiccated

color

white to tan

solubility

H2O: ≥20 mg/mL

storage temp.

2-8°C

Quality Level

Gene Information

human ... MAOB(4129)

Application

甲磺酸雷沙吉兰可被用于MAO B型介导的细胞信号转导研究。
甲磺酸雷沙吉兰已被用于:
  • 通过细胞凋亡调节因子Bax/Bcl-2的调节来检测其对视网膜色素变性(RP)的神经保护作用
  • 在1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)诱导的小鼠模型中用作单胺氧化酶-B抑制剂
  • 作为一种抗帕金森病药物,用于测试其对6-羟基多巴胺损伤的斑马鱼幼体运动迟缓和运动障碍样行为的拯救功能

Biochem/physiol Actions

抗帕金森药物;MAO B抑制剂;抗凋亡;神经保护剂
甲磺酸雷沙吉兰是单胺氧化酶的一种不可逆抑制剂,其对B型MAO的选择性比A型高十四倍。它具有抗凋亡和神经保护活性,并已被用于治疗帕金森病。
甲磺酸雷沙吉兰是帕金森病早期的一种有效治疗选择。它可改善左旋多巴治疗患者的运动波动,并对此类患者可能是一种有用辅助手段。它具有神经保护作用并可增加多巴胺能神经元的存活。

Features and Benefits

该化合物是《受体分类及信号转导》手册上多巴胺和去甲肾上腺素代谢组胺合成和代谢页面上的推荐化合物。想要浏览手册的其他页面, 请单击此处

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


历史批次信息供参考:

分析证书(COA)

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J M Rabey et al.
Clinical neuropharmacology, 23(6), 324-330 (2001-09-29)
Rasagiline mesylate (TVP-1012) is a potent, selective, non-reversible MAO-B inhibitor, without the tyramine-potentiating effect and with neuroprotective activities. The benefit of rasagiline as monotherapy in patients with early Parkinson's disease (PD) has already been reported. To evaluate the safety, tolerability
J P Finberg et al.
Neuroreport, 9(4), 703-707 (1998-04-29)
Both deprenyl and rasagiline (R(+)-N-propargyl-1-aminoindane mesylate), at a concentration of 1-10 microM, increased survival in vitro of rat E14 mesencephalic dopaminergic neurons that had been primed with 10% serum for 12 h (p < 0.05). Rasagiline, but not deprenyl, also
Rita L Vaz et al.
Pharmacology, biochemistry, and behavior, 189, 172828-172828 (2019-12-01)
Parkinson's disease (PD) is known as a movement disorder due to characteristic motor features. Existing therapies for PD are only symptomatic, and their efficacy decreases as disease progresses. Zebrafish, a vertebrate in which parkinsonism has been modelled, offers unique features
Selegiline recovers synaptic plasticity in the medial prefrontal cortex and improves corresponding depression-like behavior in a mouse model of Parkinson's disease
Okano M, et al.
Frontiers in Behavioral Neuroscience, 13, 176-176 (2019)
Dhaval R Kalaria et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 127, 204-212 (2018-02-27)
Effective treatment of Parkinson's disease (PD) involves administration of therapeutic agents with complementary mechanisms of action in order to replenish, sustain or substitute endogenous dopamine. The objective of this study was to investigate anodal co-iontophoresis of pramipexole (PRAM; dopamine agonist)

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