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SML0124

Sigma-Aldrich

Rasagiline mesylate

≥98% (HPLC)

Sinonimo/i:

(1R)-2,3-Dihydro-N-2-propynl-1H-inden-1-amine methanesulfonate, N-Propargyl-1(R)-aminoindan methanesulfonate, TVP-1012

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About This Item

Formula empirica (notazione di Hill):
C12H13N · CH4O3S
Numero CAS:
Peso molecolare:
267.34
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Stato

powder

Attività ottica

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

Condizioni di stoccaggio

desiccated

Colore

white to tan

Solubilità

H2O: ≥20 mg/mL

Temperatura di conservazione

2-8°C

Stringa SMILE

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
JDBJJCWRXSVHOQ-UTONKHPSSA-N

Informazioni sul gene

human ... MAOB(4129)

Applicazioni

Rasagiline mesylate has been used:
  • to test its neuroprotective effects in retinitis pigmentosa (RP) by apoptosis regulator, Bax/Bcl-2 modulation
  • as monoamine oxidase-B inhibitor in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induced mouse model
  • as an anti-parkinsonian agent to test its rescue functionality in 6-hydroxydopamine-lesioned zebrafish larvae towards bradykinetic and dyskinetic-like behavior

Rasagiline mesylate may be used in MAO type B-mediated cell signaling studies.

Azioni biochim/fisiol

Rasagiline mesylate is an effective therapeutic option in early stages of Parkinson′s disease. It improves the motor fluctuations in levodopa-treated patients and may be a useful adjunct to such patients. It has neuroprotective effects and increases the survival of dopaminergic neurons.
Rasagiline mesylate is an irreversible inhibitor of monoamine oxidase selective for MAO type B over type A by a factor of fourteen. It has anti-apoptotic and neuroprotectant activity and has been used as a treatment for Parkinson′s disease.

Caratteristiche e vantaggi

This compound is featured on the Dopamine and Norepinephrine Metabolism and Histamine Synthesis and Metabolism pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pittogrammi

Exclamation mark

Avvertenze

Warning

Indicazioni di pericolo

Classi di pericolo

Acute Tox. 4 Oral

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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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
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)
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
O Rascol et al.
Lancet (London, England), 365(9463), 947-954 (2005-03-16)
Rasagiline mesylate is a novel drug for Parkinson's disease with selective, irreversible monoamine oxidase B (MAO-B) inhibitor activity, and is effective as monotherapy in early disease. This study investigated rasagiline efficacy and safety in levodopa-treated patients with Parkinson's disease and

Articoli

Serotonin (5-hydroxytryptamine) is principally found stored in three main cell types - i) serotonergic neurons in the CNS and in the intestinal myenteric plexus, ii) enterochromaffin cells in the mucosa of the gastrointestinal tract, and iii) in blood platelets. Metabolism of serotonin is carried out primarily by the outer mitochondrial membrane enzyme monoamine oxidase (MAO), which occurs as two molecular subtypes called MAO-A and MAO-B.

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