|(S)-2-(4-(3-氟苄氧基)苄氨基)丙基酰胺|CsnPharm

CAS No.: 133865-89-1

沙芬酰胺 Catalog No. CSN11880

Synonyms: FCE 26743;EMD 1195686;FCE-28073

Safinamide is a reversible and highly selective MAO-B inhibitor with IC50 of 98 nM.

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生物活性

描述Glial cells contain two enzymes that metabolize biogenicamines: COMT and MAO. MAO, located in the outer mitochondrial membrane, occurs as two isozymes: A and B. MAO-A is predominantly found in the intestinal tract and, in the CNS, presynaptic neurons; MAO-B is mainly located in the brain, generally in glial cells near dopaminergic synapses. MAO-B regulates the free concentrations of biogenic amines in the synaptic cleft^[3].Safinamide is a highly selective and reversible MAO-B inhibitor that produces an increase in extracellular levels of dopamine in the striatum^[4]. The non-dopaminergic mechanism of action involves state- and use-dependent blockade of voltagegated sodium channels and modulation of N-type calcium channels, thereby inhibiting glutamate release^[5]. In rats, safinamide was &5000-fold more potent in inhibiting MAO-B than MAO-A ^[6]. In humans, safinamide provided platelet MAO-B inhibition at doses of C0.5 mg/kg,but did not inhibit MAO-A enzyme activity at a dose of 10 mg/kg^[7].Safinamide has demonstrated neuroprotective, neurorescuing, anti-inflammatory and tremorolytic properties in several animal models,and was shown to reduce the duration and intensity of levodopa-induced dyskinesia in parkinsonian monkeys^[8]. in vitro , safinamide is not a substrate for the transporters P-glycoprotein, BCRP, OAT1B1, OAT1B3, OATP1A2 or OATP2B1. The metabolite safinamide acid is not a substrate for OCT2 or OAT1 but is a substrate for OAT3,although potential pharmacokinetic interactions are not likely to be clinically relevant. Safinamide acid does not inhibit OCT2, MATE1 or MATE2-K^[9].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00627640	Idiopathic Parkinson's Disease	Phase 3	Completed	-	-
NCT00642889	Parkinson's Disease	Phase 3	Completed	-	-
NCT01028586	Idiopathic Parkinson's Disease	Phase 3	Terminated(Trial is terminated... more >> due to a company decision to return all rights for Safinamide back to Newron Pharmaceuticals) Collapse <<	-	Switzerland ... more >> Enquire Central Contact Geneva, Switzerland Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3075 mL
- 16.5375 mL
- 33.0750 mL
- 5 mM
- 0.6615 mL
- 3.3075 mL
- 6.6150 mL
- 10 mM
- 0.3307 mL
- 1.6537 mL
- 3.3075 mL

技术信息

CAS号

133865-89-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H19FN2O2

运输

蓝冰

分子量

302.34

别名

FCE 26743;EMD 1195686;FCE-28073;NW-1015;PNU-151774E;Xadago;沙芬酰胺

溶解度

DMSO	59.0 mg/mL (195.1 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00627640	Idiopathic Parkinson's Disease	Phase 3	Completed	-	-
NCT00642889	Parkinson's Disease	Phase 3	Completed	-	-
NCT01028586	Idiopathic Parkinson's Disease	Phase 3	Terminated(Trial is terminated... more >> due to a company decision to return all rights for Safinamide back to Newron Pharmaceuticals) Collapse <<	-	Switzerland ... more >> Enquire Central Contact Geneva, Switzerland Collapse <<
NCT01187966	Parkinson's Disease	Phase 3	Completed	-	-
NCT01286935	Parkinson's Disease	Phase 3	Completed	-	-
NCT03648671	-	-	Recruiting	November 30, 2019	Italy ... more >> Azienda ospedaliera universitaria integrata verona Recruiting Verona, Italy, 37126 Contact: Michele Tinazzi, MD, PhD 0458027472 michele.tinazzi@univr.it Collapse <<
NCT00865579	Parkinson's Disease	Phase 3	Terminated(study terminated ea... more >>rly due to change in Sponsorship) Collapse <<	-	Romania ... more >> Research Site Timis, Romania Collapse <<
NCT00605683	Idiopathic Parkinson's Disease	Phase 3	Completed	-	-
NCT00643045	Idiopathic Parkinson's Disease	Phase 3	Completed	-	-
NCT01026428	Idiopathic Parkinson's Disease	Phase 1 Phase 2	Completed	-	Italy ... more >> Research Site Casino, Italy Research Site Roma, Italy Collapse <<
NCT01027169	Hepatic Impairment	Phase 1	Completed	-	Germany ... more >> CRS Clinical Research Services Kiel GmbH Kiel, Germany Collapse <<
NCT03753763	Multiple System Atrophy	Phase 2	Not yet recruiting	March 31, 2020	-
NCT01264861	Parkinson Disease	Phase 2	Terminated(The Dopamine transp... more >>orter brain imaging trial is terminated due to a company decision to return all rights for Safinamide back to Newron Pharmaceuticals) Collapse <<	-	United States, Connecticut ... more >> Molecular Neuroimaging, LLC New Haven, Connecticut, United States, 06510 Collapse <<
NCT02495831	Healthy	Phase 1	Completed	-	Switzerland ... more >> Cross Research SA, Phase I Unit Arzo, Ticino, Switzerland, 6864 Collapse <<
NCT01211587	Parkinson's Disease With Cogni... more >>tive Impairments Collapse <<	Phase 2	Completed	-	United States, California ... more >> The Parkinson's Institute Sunnyvale, California, United States United States, Florida Mayo Clinic Florida Jacksonville, Florida, United States United States, Georgia Emory University Atlanta, Georgia, United States United States, Illinois Northwestern University Chicago, Illinois, United States Rush University Medical Center Chicago, Illinois, United States United States, Maryland Johns Hopkins University Baltimore, Maryland, United States United States, Massachusetts US Medical Information Located in Rockland, Massachusetts, United States United States, Ohio Cleveland Clinic Cleveland, Ohio, United States United States, Texas Baylor College of Medicine Parkinson's Disease Center and Movement Disorders Clinic Houston, Texas, United States Spain Hospital Clinic de Barcelona Barcelona, Spain Hospital De La Santa Creui Sant Pau Barcelona, Spain Hospital General de Catalunya Barcelona, Spain USP Institut Universitari Dexeus Barcelona, Spain Hosptial General Univ Gregorio Maranon Madrid, Spain Hospital Mutual de Terrassa Terrassa - Barcelona, Spain Collapse <<
NCT03216304	Healthy	Phase 1	Completed	-	Switzerland ... more >> CROSS Research SA, Phase I Unit Arzo, Ticino, Switzerland, 6864 Collapse <<
NCT02495831	-	-	Completed	-	-
NCT01113320	Parkinson's Disease	Phase 2	Completed	-	Austria ... more >> Medical University Graz, Klinische Abteilung für Spezielle Neurologie Graz, Austria Medical University Innsbruck, Dept. of Neurology Innsbruck, Austria Canada Quebec Memory and Motor Skills Disorders Quebec, Canada France Hôpital Roger Sallengro Lille, France CIC-Hospital Purpan Toulouse, France Germany Neurologie Berlin Praxen Berlin, Germany St. Josef Hospital, Klinik für Neurologie Bochum, Germany Facharzt für Neurologie und Psychiatrie Düsseldorf, Germany South Africa Medical and Dental center (ZAF) Johannesbourg, South Africa Sunninghill Hospital Johannesburg, South Africa Willows Medical Centre Pretoria, South Africa Collapse <<
NCT01374113	Renal Impairment	Phase 1	Completed	-	Germany ... more >> CRS Clinical Research Services Kiel GmbH Kiel, Schleswig-Holstein, Germany Collapse <<

沙芬酰胺 Catalog No. CSN11880

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