Rasagiline mesylate

Rasagiline mesylate Struktur
161735-79-1
CAS-Nr.
161735-79-1
Englisch Name:
Rasagiline mesylate
Synonyma:
Azilect;RASAGILINE MESILATE;RASAGILINE GLUCURONIDE;CS-289;TVP-101;Agilect;TV 1012;TVP-1012;Unii-lh8C2ji290;RASAGILINE MESYLATE
CBNumber:
CB7501001
Summenformel:
C13H17NO3S
Molgewicht:
267.34398
MOL-Datei:
161735-79-1.mol

Rasagiline mesylate Eigenschaften

Schmelzpunkt:
155-158°C
storage temp. 
2-8°C
Löslichkeit
H2O: ≥20mg/mL
Aggregatzustand
powder
Farbe
white to tan
Optische Aktivität
[α]/D +15 to +28°, c = 0.6 mg/mL in H2O
Stabilität:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO, distilled water or ethanol may be stored at -20°C for up to 1 month.
InChI
InChI=1/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-;/s3
InChIKey
JDBJJCWRXSVHOQ-ZLBVLXFENA-N
SMILES
C12C=CC=CC=1CC[C@H]2NCC#C.S(C)(O)(=O)=O |&1:8,r|
CAS Datenbank
161735-79-1(CAS DataBase Reference)
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
Kennzeichnung gefährlicher Xn
R-Sätze: 22
S-Sätze: 24/25
WGK Germany  3
HS Code  29214990
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitsschädlich bei Verschlucken. Akute Toxizität oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
Sicherheit
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Rasagiline mesylate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Rasagiline mesylate is a potent and selective irreversible monoamine oxidase B (MAO-B) inhibitor launched in 2005 in Israel by Teva as monotherapy in patients with early Parkinson's disease and as adjuvant treatment in moderate-toadvanced disease. Lundbeck will market the drug throughout Europe. Rasagiline is in phase II clinical trials at Teva and Eisai for the treatment of Alzheimer's type dementia.

Chemische Eigenschaften

White to Off-White Crystalline Solid

Verwenden

Rasagiline Mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Indications

Rasagiline mesylate is a novel, potent, second-generation, selective, irreversible MAO-B inhibitor that blocks the breakdown of dopamine. It is approved for the treatment of PD. Indications for use of once-daily rasagiline are as a monotherapy in early PD and as an adjunct to levodopa in moderate to advanced disease. Rasagiline significantly improves symptoms during initial monotherapy in patients with early PD and as an adjunct treatment to levodopa in moderate-to-advanced patients. Rasagiline is well tolerated up to doses as high as 20 mg/day. Evidence for neuroprotective effect of rasagiline is as follows (Jain 2010c):
Structure activity studies have shown that the neuroprotective activity is associated with the propargyl moiety of rasagiline, which protects mitochondrial viability.
Experimental evidence supports rasagiline's neuroprotective efficacy, showing that neuronal survival is related to the anti-apoptotic properties of its propargyl moiety. Aminoindan metabolite of rasagiline has been shown to have neuroprotective properties (Bar-Am et al. 2010).

Allgemeine Beschreibung

Rasagiline mesylate, (R)-N-(prop-2-ynyl)-2,3-dihydro-1H-inden-1-amine methanesulfonate(Azilect), belongs to the propargylamine family and is a whiteto off-white powder, soluble in water or ethanol, slightly solublein isopropanol. Rasagiline is rapidly absorbed. Plasmaprotein binding for rasagiline ranges from 88% to 94%, withspecific binding to serum albumin being 61% to 63%. It undergoescomplete biotransformation before excretion, mainlyvia N-dealkylation and hydroxylation, to yield three majormetabolites: 1(R)-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, and 3-hydroxy-1-aminoindan. Both oxidativepathways are catalyzed by cytochrome P450 (CYP) enzymes,mainly the 1A2 isozyme. Rasagiline and its metabolites undergoglucuronide conjugation with subsequent urinary excretion.Inhibitors of the CYP1A2 may increase plasmaconcentrations of rasagiline up to twofold. Because rasagilineis a selective and irreversible inhibitor of MAO-B, itsduration of action is independent of the drug’s half-life and isinstead determined by the regeneration rate of MAO-B. Thischaracteristic is potentially beneficial in PD, where rasagiline’sprolonged effect may be able to limit the fluctuating responsesthat are characteristic of long-term drug treatmentwith levodopa.

Mechanism of action

The specific mechanism of action of Rasagiline mesylate is unknown. One of these mechanisms is thought to be related to its MAO-B inhibitory activity, which leads to elevated extracellular dopamine levels in the striatum. It irreversibly blocks dopamine metabolism, thereby increasing dopamine levels, which can be beneficial for symptoms in Parkinson's disease patients.

Rasagiline mesylate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Rasagiline mesylate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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161735-79-1()Verwandte Suche:


  • N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate
  • Rasagiline Mesylate/Tartrate/Base
  • (1R)-2,3-Dihydro-N-2-propyn-1-yl-1H-inden-1-amine Mesylate
  • (R)-N-2-Propynyl-1-indanamine Mesylate
  • Agilect
  • TVP-101
  • RASAGILINE MESYLATE
  • (r)-n-2-propynyl-1-indanamine methanesulfonate
  • Rasagiline nesylate
  • TVP-1012
  • (R)-2,3-Dihydro-N-2-propynyl-1-indenaMine Mesylate
  • TV 1012
  • (R)-N-(Prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-aMine Methanesulfonate
  • (1R)-2,3-dihydro-N-2-propyn-1-yl-1H-inden-1-amine,methanesulfonate (1:1)
  • (1R)-2,3-Dihydro-N-2-propynl-1H-inden-1-amine methanesulfonate
  • N-Propargyl-1(R)-aminoindan methanesulfonate
  • 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (R)-, methanesulfonate
  • Rasagiline methanesulfonate
  • Unii-lh8C2ji290
  • Rasagiline Mesylate(pure)
  • Rasagiline MesylateQ: What is Rasagiline Mesylate Q: What is the CAS Number of Rasagiline Mesylate Q: What is the storage condition of Rasagiline Mesylate Q: What are the applications of Rasagiline Mesylate
  • (1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine methanesulfonate
  • CS-289
  • R-(+)-Rasagiline mesylate
  • 1H-Inden-1-amine, 2,3-dihydro-N-2-propyn-1-yl-, (1R)-, methanesulfonate (1:1)
  • (R)-N-(2-Propyn-1-yl)-1-indanamine Methanesulfonate
  • (R)-N-Propargyl-1-indanamine Methanesulfonate
  • Rasagiline mesylate USP/EP/BP
  • Azilect
  • RASAGILINE MESILATE
  • RASAGILINE GLUCURONIDE
  • (1R)-N-prop-2-ynylindan-1-amine
  • Resagiline mesylate
  • 161735-79-1
  • 136235-79-1
  • 161735-79-5
  • C12H13NCH4O3S
  • Chiral
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Rasagiline
  • Signalling
  • APIs
  • 161735-79-1
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