メシル酸ラサジリン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

• 注意書き

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

メシル酸ラサジリン 価格

メシル酸ラサジリン 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 効能

  パーキンソン病治療薬, モノアミン酸化酵素B(MAO-B)阻害薬

• 商品名

  アジレクト (武田薬品工業)

• 説明

  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.

• 化学的特性

  White to Off-White Crystalline Solid

• 使用

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

• 適応症

  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).

• 一般的な説明

  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.

• 作用機序

  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.

メシル酸ラサジリン 上流と下流の製品情報

メシル酸ラサジリン 生産企業

Global(391)Suppliers

メシル酸ラサジリン スペクトルデータ(¹HNMR)

161735-79-1, メシル酸ラサジリン キーワード