Safinamide

MAO-B inhibitor CAS# 133865-89-1

Safinamide

Catalog No. BCC1915----Order now to get a substantial discount!

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Chemical structure

Safinamide

3D structure

Chemical Properties of Safinamide

Cas No. 133865-89-1 SDF Download SDF
PubChem ID 5487407 Appearance Powder
Formula C17H19FN2O2 M.Wt 302.34
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EMD 1195686; FCE 26743
Solubility Soluble in DMSO
Chemical Name (2R)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methylamino]propanamide
SMILES CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F
Standard InChIKey NEMGRZFTLSKBAP-GFCCVEGCSA-N
Standard InChI InChI=1S/C17H19FN2O2/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14/h2-9,12,20H,10-11H2,1H3,(H2,19,21)/t12-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Safinamide

DescriptionSafinamide (EMD 1195686; FCE 26743) selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A. IC50 value: 98 nM [1] Target: MAO-B Safinamide (EMD 1195686; FCE 26743; ) is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, Safinamide (EMD 1195686; FCE 26743; ) is voltage-dependent sodium and calcium channel blocker. Safinamide (EMD 1195686; FCE 26743; ) appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.

References:
[1]. Leonetti F, et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem, 2007, 50(20), 4909-4916. [2]. Schapira AH. Safinamide in the treatment of Parkinson's disease. Expert Opin Pharmacother. 2010 Sep;11(13):2261-8. [3]. Onofrj M, et al. An expert opinion on safinamide in Parkinson's disease. Expert Opin Investig Drugs. 2008 Jul;17(7):1115-25. [4]. Chazot PL. Safinamide for the treatment of Parkinson's disease, epilepsy and restless legs syndrome. Curr Opin Investig Drugs. 2007 Jul;8(7):570-9. [5]. Dal Bo L, et al. Bioassay of safinamide in biological fluids of humans and various animal species. Arzneimittelforschung. 2006;56(12):814-9. http://www.ncbi.nlm.nih.gov/pubmed/17260668

Safinamide Dilution Calculator

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Safinamide Molarity Calculator

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Preparing Stock Solutions of Safinamide

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.3075 mL 16.5377 mL 33.0753 mL 66.1507 mL 82.6884 mL
5 mM 0.6615 mL 3.3075 mL 6.6151 mL 13.2301 mL 16.5377 mL
10 mM 0.3308 mL 1.6538 mL 3.3075 mL 6.6151 mL 8.2688 mL
50 mM 0.0662 mL 0.3308 mL 0.6615 mL 1.323 mL 1.6538 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.6615 mL 0.8269 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Safinamide

Safinamide (EMD 1195686; FCE 26743; ) is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, Safinamide (EMD 1195686; FCE 26743; ) is voltage-dependent sodium and calcium channel blocker. Safinamide (EMD 1195686; FCE 26743; ) appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.

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References on Safinamide

Identification, Characterization, and Quantification of Impurities of Safinamide Mesilate: Process-Related Impurities and Degradation Products.[Pubmed:28150570]

J AOAC Int. 2017 Jul 1;100(4):1029-1037.

The characterization of process-related impurities and degradation products of Safinamide mesilate (SAFM) in bulk drug and a stability-indicating HPLC method for the separation and quantification of all the impurities were investigated. Four process-related impurities (Imp-B, Imp-C, Imp-D, and Imp-E) were found in the SAFM bulk drug. Five degradation products (Imp-A, Imp-C, Imp-D, Imp-E, and Imp-F) were observed in SAFM under oxidative conditions. Imp-C, Imp-D, and Imp-E were also degradation products and process-related impurities. Remarkably, one new compound, identified as (S)-2-[4-(3-fluoro-benzyloxy) benzamido] propanamide (i.e., Imp-D), is being reported here as an impurity for the first time. Furthermore, the structures of the aforementioned impurities were characterized and confirmed via IR, NMR, and MS techniques, and the most probable formation mechanisms of all impurities proposed according to the synthesis route. Optimum separation was achieved on an Inertsil ODS-3 column (250 x 4.6 mm, 5 mum), using 0.1% formic acid in water (pH adjusted to 5.0) and acetonitrile as the mobile phase in gradient mode. The proposed method was found to be stability-indicating, precise, linear, accurate, sensitive, and robust for the quantitation of SAFM and its process-related substances, including its degradation products.

Effects of Safinamide on Pain in Fluctuating Parkinson's Disease Patients: A Post-Hoc Analysis.[Pubmed:27802242]

J Parkinsons Dis. 2017;7(1):95-101.

BACKGROUND: Pain, a frequent non-motor symptom in Parkinson's Disease (PD), significantly impacts on quality of life. Safinamide is a new drug with dopaminergic and non-dopaminergic properties, approved in Europe as adjunct therapy to levodopa for the treatment of fluctuating PD patients. Results from two 24-month, double-blind, placebo-controlled studies demonstrated that Safinamide has positive effects on both motor functions and quality of life in PD patients. OBJECTIVE: To investigate the effects of Safinamide on pain management in PD patients with motor fluctuations using pooled data from studies 016 and SETTLE. METHODS: This post-hoc analysis evaluated the reduction of concomitant pain treatments and the changes in the scores of the items related to pain of the Parkinson's Disease Quality of Life Questionnaire (PDQ-39). A path analysis was performed in order to examine direct and indirect associations between Safinamide and PDQ-39 pain-related items assessed after 6-months of treatment. RESULTS: The percentage of patients with no pain treatments at the end of the trials was significantly lower in the Safinamide group compared to the placebo group. Safinamide 100 mg/day significantly reduced on average the individual use of pain treatments by approximately 24% and significantly improved two out of three PDQ-39 pain-related items of the "Bodily discomfort" domain.Path analysis showed that the direct effect of Safinamide on pain accounted for about 80% of the total effect. CONCLUSIONS: These results suggest that Safinamide may have a positive effect on pain, one of the most underestimated non-motor symptoms. Prospective studies are warranted to investigate this potential benefit.

Safinamide: A Review in Parkinson's Disease.[Pubmed:28110399]

CNS Drugs. 2017 Feb;31(2):169-176.

Safinamide (Xadago((R))) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. In the EU, Safinamide is approved for the treatment of mid- to late-stage fluctuating Parkinson's disease (PD) as add-on therapy to a stable dose of levodopa alone or in combination with other PD medications. Safinamide 50-100 mg/day administered as a fixed or flexible dose significantly increased daily 'on' time without dyskinesia (primary endpoint) in patients with mid- to late-stage PD with motor fluctuations in 24-week, placebo-controlled clinical trials. Other outcomes, including motor function, overall clinical status and health-related quality of life, were also generally improved with Safinamide. Furthermore, in an 18-month extension of one study, although dyskinesia (primary endpoint) was not significantly improved with Safinamide relative to placebo, treatment benefits in other outcomes were generally sustained over 24 months of treatment. Safinamide was generally well tolerated in clinical trials; dyskinesia was the most common adverse event. Although further studies are needed, including comparative and long-term studies, current evidence indicates that Safinamide extends the treatment options available for use as add-on therapy to levodopa and other PD medications in patients with mid- to late-stage PD experiencing motor fluctuations.

Assessment of Safety and Efficacy of Safinamide as a Levodopa Adjunct in Patients With Parkinson Disease and Motor Fluctuations: A Randomized Clinical Trial.[Pubmed:27942720]

JAMA Neurol. 2017 Feb 1;74(2):216-224.

Importance: Although levodopa remains the most effective oral pharmacotherapy for Parkinson disease (PD), its use is often limited by wearing off effect and dyskinesias. Management of such complications continues to be a significant challenge. Objective: To investigate the efficacy and safety of Safinamide (an oral aminoamide derivative with dopaminergic and nondopaminergic actions) in levodopa-treated patients with motor fluctuations. Design, Setting, and Participants: From March 5, 2009, through February 23, 2012, patients from academic PD care centers were randomized (1:1 ratio) to receive double-blind adjunctive Safinamide or placebo for 24 weeks. All patients had idiopathic PD with "off" time (time when medication effect has worn off and parkinsonian features, including bradykinesia and rigidity, return) of greater than 1.5 hours per day (excluding morning akinesia). Their pharmacotherapy included oral levodopa plus benserazide or carbidopa in a regimen that had been stable for 4 weeks or longer. During screening, each patient's regimen was optimized to minimize motor fluctuations. Study eligibility required that after 4 weeks of optimized treatment, the patients still have more than 1.5 hours per day of off time. Adverse events caused the premature study discontinuation of 12 individuals (4.4%) in the Safinamide group and 10 individuals (3.6%) in the placebo group. Interventions: Patients took Safinamide or placebo as 1 tablet daily with breakfast. If no tolerability issues arose by day 14, the starting dose, 50 mg, was increased to 100 mg. Main Outcomes and Measures: The prespecified primary outcome was each treatment group's mean change from baseline to week 24 (or last "on" treatment value) in daily "on" time (relief of parkinsonian motor features) without troublesome dyskinesia, as assessed from diary data. Results: At 119 centers, 549 patients were randomized (mean [SD] age, 61.9 [9.0] years; 334 male [60.8%] and 371 white [67.6%]): 274 to Safinamide and 275 to placebo. Among them, 245 (89.4%) receiving Safinamide and 241 (87.6%) receiving placebo completed the study. Mean (SD) change in daily on time without troublesome dyskinesia was +1.42 (2.80) hours for Safinamide, from a baseline of 9.30 (2.41) hours, vs +0.57 (2.47) hours for placebo, from a baseline of 9.06 (2.50) hours (least-squares mean difference, 0.96 hour; 95% CI, 0.56-1.37 hours; P < .001, analysis of covariance). The most frequently reported adverse event was dyskinesia (in 40 [14.6%] vs 15 [5.5%] and as a severe event in 5 [1.8%] vs 1 [0.4%]). Conclusions and Relevance: The outcomes of this trial support Safinamide as an effective adjunct to levodopa in patients with PD and motor fluctuations to improve on time without troublesome dyskinesia and reduce wearing off. Trial Registration: clinicaltrials.gov Identifier NCT00627640.

Description

Safinamide (EMD 1195686; FCE 26743) selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A.

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