リバスチグミン
リバスチグミン 物理性質
- 比旋光度 :
- D20 -32.1° (c = 5 in ethanol)
- 沸点 :
- 316.2±34.0 °C(Predicted)
- 比重(密度) :
- 1.038±0.06 g/cm3(Predicted)
- 闪点 :
- 145℃
- 貯蔵温度 :
- Sealed in dry,Store in freezer, under -20°C
- 溶解性:
- Chloroform (Sparingly), Ethyl Acetate (Slightly)
- 外見 :
- Powder
- 酸解離定数(Pka):
- pKa 8.99 (Uncertain)
- CAS データベース:
- 123441-03-2(CAS DataBase Reference)
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01W0118-0285 |
リバスチグミン 90.0+% (HPLC)
Rivastigmine 90.0+% (HPLC) |
123441-03-2 |
50mg |
￥23000 |
2018-12-26 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01W0118-0285 |
リバスチグミン 90.0+% (HPLC)
Rivastigmine 90.0+% (HPLC) |
123441-03-2 |
250mg |
￥68000 |
2018-12-26 |
購入 |
|
Sigma-Aldrich Japan
|
PHR3343 |
certified reference material, pharmaceutical secondary standard
Rivastigmine certified reference material, pharmaceutical secondary standard |
123441-03-2 |
0.2ML |
￥28900 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
1604836 |
United States Pharmacopeia (USP) Reference Standard
Rivastigmine United States Pharmacopeia (USP) Reference Standard |
123441-03-2 |
0.1ml |
￥58400 |
2024-03-01 |
購入 |
リバスチグミン 化学特性,用途語,生産方法
外観
無色～褐色、澄明の液体
溶解性
エタノールに可溶(10mg/ml：ほとんど澄明以内)
用途
強力なコリンエステラーゼ及
びブチリルコリンエステラーゼの阻害剤で
す。
効能
認知症治療薬, アセチルコリンエステラーゼ阻害薬
商品名
イクセロン (ノバルティスファーマ); リバスタッチ (小野薬品工業)
使用上の注意
不活性ガス封入
使用
Antidepressant
定義
ChEBI: A carbamate ester obtained by formal condensation of the carboxy group of ethyl(methyl)carbamic acid with the phenolic OH group of 3-[(1S)-1-(dimethylamino)ethyl]phenol. A reversible cholinesterase inhibitor.
一般的な説明
Rivastigmine (Exelon, EA 713) is apseudoirreversible noncompetitive carbamate inhibitor ofAChE. Although the half-life is approximately 2 hours,the inhibitory properties of this agent last for 10 hours becauseof the slow dissociation of the drug from the enzyme.The Food and Drug Administration (FDA) approved its usein mild-to-moderate Alzheimer disease in April 2000. InJuly 2007, rivastigmine was granted approval for use inmanaging mild-to-moderate dementia associated withParkinson disease.
薬物動態学
Rivastigmine is a centrally selective, arylcarbamate AChEI that was approved in 2000 for oral administration in the treatment of AD. It has an
elimination half-life of 1.4 to 1.7 hours but is able to inhibit AChE for up to 10 hours. Because of the slow dissociation of the carbamylated
enzyme, it has been referred to as a pseudo-irreversible AChEI. Like donepezil, rivastigmine exhibits a low level of hepatotoxicity. It is
rapidly and extensively hydrolyzed in the CNS by cholinesterase with minimal involvement of CYP450. The phenolic metabolite is excreted
primarily via the kidneys.
代謝
Rivastigmine is the tertiary amines that
are rapidly absorbed from the gastrointestinal tract, as
are tacrine, donepezil, and galanthamine, whereas quaternary
ammonium compounds are poorly absorbed
after oral administration. Nevertheless, quaternary ammonium
compounds like neostigmine and pyridostigmine
are orally active if larger doses are employed.
Only the quaternary ammonium inhibitors do not readily
enter the CNS. Because of their high lipid solubility
and low molecular weight, most of the organophosphates
are absorbed by all routes of administration;
even percutaneous exposure can result in the absorption
of sufficient drug to permit the accumulation of
toxic levels of these compounds.
リバスチグミン 上流と下流の製品情報
原材料
準備製品
リバスチグミン 生産企業
Global( 309)Suppliers
123441-03-2(リバスチグミン)キーワード:
- 123441-03-2
- (S)-N-Ethyl-N-Methyl- 3-[1-(diMethylaMino)ethyl]- phenyl carbaMate
- S-RivastigMine
- CarbaMic acid, N-ethyl-N-Methyl-, 3-[(1S)-1-(diMethylaMino)ethyl]phenyl ester
- RivastigiMine
- (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate
- Revastigmine
- N-Ethyl-N-methylcarbamic acid 3-[(1S)-1-(dimethylamino)ethyl]phenyl-ester
- Revastigmine (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate
- Rivastigmine Base/ Tartrate
- RIVASTIGMINE
- RIVASTIGIMINE(FORR&DONLY)
- 3-((1S)-1-(Dimethylamino)ethyl)phenyl N-ethyl-N-methylcarbamate
- Ethylmethylcarbamic acid 3-((1S)-1-(dimethylamino)ethyl)phenyl ester
- 3-((1S)-1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
- Carbamic acid, ethylmethyl-, 3-((1S)-1-(dimethylamino)ethyl)phenyl ester
- Carbamic acid, ethylmethyl-, 3-(1-(dimethylamino)ethyl)phenyl ester, (S)-
- Ena 713 free base
- Unii-pki06m3iw0
- Rivastigmine (0.1 mL)
- (S)-3-[1-(diMethylaMino)ethyl]phenyl N-ethyl-N-MethylcarbaMate
- bis(sulfanylidene)ruthenium
- Rivastigmine for system suitability CRS
- Rivastig
- Rivastigmine USP/EP/BP
- Rivastigmine intermediate,Rivastigmine
- Rivastigmine (1604836)
- EXELON
- RIVASTIGMINE HYDROGEN TARTRATE
- Rivastigmine base
- mine
- リバスチグミン
- リバスチグミン (JAN)
- N-エチル-N-メチルカルバミド酸3-[(1S)-1-(ジメチルアミノ)エチル]フェニル
- 3-[(1S)-1-(ジメチルアミノ)エチル]フェニル N-エチル-N-メチルカルバマート
- メチルエチルカルバミド酸3-[(S)-1-(ジメチルアミノ)エチル]フェニル
- (S)-リバスチグミン
- リバスティグミン
- N-エチル-N-メチルカルバミド酸3-[(S)-1-(ジメチルアミノ)エチル]フェニル
- イクセロン
- リバスタッチ
- エチルメチルカルバミド酸3-[(S)-1-(ジメチルアミノ)エチル]フェニル