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Rasagiline

Names

[ CAS No. ]:
136236-51-6

[ Name ]:
Rasagiline

[Synonym ]:
(1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine
(1R)-N-(Prop-2-yn-1-yl)indan-1-amine
(1R)-N-(2-Propyn-1-yl)-1-indanamine
(1R)-N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine
Rasagiline
1H-Inden-1-amine, 2,3-dihydro-N-2-propyn-1-yl-, (1R)-
(1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine
(R)-N-(2-Propynyl)-2,3-dihydroinden-1-amine

Biological Activity

[Description]:

Rasagiline(AGN1135;TVP1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease. Target: Monoamine Oxidase (MAO)-BRasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as monotherapy or adjunct to L-Dopa for patients with early and late Parkinson's disease (PD) [1]. Rasagiline inhibits MAO-B more potently than selegiline and has the advantage of once-daily dosing. In several large, randomized, placebo-controlled trials, rasagiline has demonstrated efficacy as monotherapy in early PD and as adjunctive therapy in advanced PD. In addition, rasagiline has been shown to have neuroprotective effects in in vitro and in vivo studies. The recently completed delayed-start ADAGIO (Attenuation of Disease Progression with Azilect Given Once-daily) trial suggests a potential disease-modifying effect for rasagiline 1 mg/day, though the clinical import of this finding has yet to be established [2]. Rasagiline has been found to be well tolerated and effective in the treatment of early PD and as adjunctive treatment in motor fluctuations. Whether rasagiline is associated with clinically significant neuroprotection (ie, disease modification) in PD is the subject of ongoing clinical trials [3].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase
Research Areas >> Neurological Disease

[References]

[1]. Leegwater-Kim, J. and E. Bortan, The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging, 2010. 5: p. 149-56.

[2]. Weinreb, O., et al., Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol, 2010. 92(3): p. 330-44.

[3]. Chen, J.J., D.M. Swope, and K. Dashtipour, Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther, 2007. 29(9): p. 1825-49.


[Related Small Molecules]

Phenelzine (sulfate) | trans-2-Phenylcyclopropylamine hemisulfate salt | Clorgyline hydrochloride | Rosmarinic acid | pargyline hydrochloride | GSK-LSD1 Dihydrochloride | Rasagiline mesylate | Mofegiline hydrochloride | Paeonol | Iproniazid (phosphate) | Safinamide | TVP1022 | Minaprine | Nialamide | Desmethoxyyangonin

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
305.5±30.0 °C at 760 mmHg

[ Melting Point ]:
35-41°C

[ Molecular Formula ]:
C12H13N

[ Molecular Weight ]:
171.238

[ Flash Point ]:
146.8±20.0 °C

[ Exact Mass ]:
171.104797

[ PSA ]:
12.03000

[ LogP ]:
2.27

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.577

[ Storage condition ]:
2-8°C

MSDS

Safety Information

[ Hazard Codes ]:
Xi

[ HS Code ]:
2921499090

Synthetic Route

Precursor & DownStream

Customs

[ HS Code ]: 2921499090

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%


Related Compounds