ジギトキシン 化学特性,用途語,生産方法
外観
白色~ほとんど白色, 粉末
溶解性
エタノールに微溶。クロロホルムに可溶。水, エチルエーテルに不溶。エタノールにやや溶けにくく、水及びアセトンにほとんど溶けない。
解説
ジギトキシン,融点257 ℃.[α]D20"+4.8°(ジオキサン).1 g は約40 mL のクロロホルム,約60 mL のエタノールに溶ける.水に難溶.原配糖体ラナトシドA(ジギラニド)をアルカリ加水分解後,ジギラニダーゼで酵素分解するとジギトキシンを与える.強心作用を示し,強心薬(うっ血性心不全,頻脈などの治療)に使用される.
用途
薬理・生理作用研究用。
用途
強心配糖体剤です。Na+、K+-
ATPase 阻害作用を示します。
用途
強心配糖体剤です。Na+、K+ATPase阻害作用を示します。
製法
酸で加水分解され,ジギトキシゲニン(1分子),D-ジギトキソース(3分子)を生じる.糖部はアグリコンの3位についているジギトキシン.
効能
強心薬
毒性
LD50 0.18 mg/kg(ネコ)
説明
Digitoxin is the most powerful and reliable of the glucosides which have been extracted from digitalis leave. It is a cardiac glycoside (CG). It is a cardiotonic drug, which exhibits cardiac and anti-cancer properties. Digitoxin inhibits nuclear factor kappa B (NF-κB) signaling. It is used to treat congestive heart failure and cardiac arrhythmia. Digitoxin prevents microtubule formation.
化学的特性
White Solid
使用
Digitoxin has been used as a labeled drugs for binding sites on human serum albumin (HSA). It has also been used to test its anti-transmissible gastroenteritis virus (TGEV) activity.
適応症
Digitoxin (Dig) is an FDA approved drug for the treatment of cardiac disease.
Digitoxin is used for the treatment of heart failure, especially in people with impaired kidney function. It is also used to treat certain kinds of heart arrhythmia, such as atrial fibrillation.
Digoxin is used to treat heart failure and abnormal heart rhythms (arrhythmias). It also helps the heart work better and control heart rate. Digoxin may be used after a heart attack. This medication comes in various forms: tablet, capsule, or pediatric elixir (liquid). It is available under the brand names Lanoxin, Cardoxin, Digitek, Digox, and Lanoxicaps.
一般的な説明
Odorless white or pale buff microcrystalline powder. Used as a cardiotonic drug.
健康ハザード
Material is bioactive and capable of causing cardiac arrythmias and electrolyte imbalances that may be fatal. Death is due to ventricular fibrillation or cardiac standstill. Material has a high toxicity hazard rating; it may cause death or permanent injury after a very short exposure. It is classified as super toxic; an estimated single lethal dose is 3-10 mg.
火災危険
When heated to decomposition, DIGITOXIN emits acrid smoke and irritating fumes.
安全性プロファイル
A deadly poison by
most routes. Human systemic effects:
arrhythmias, cardiomyopathy, EKG
changes, nausea or vomiting, paresthesia,
pulse rate increase, thrombocytopenia.
Human reproductive effects by ingestion:
reduced viability of newborn. An eye irritant. When heated to decomposition it
emits acrid smoke and irritating fumes. See
also DIGITALIS.
純化方法
Digitoxin crystallises from MeOH, aqueous EtOH with 0.5 to 1 H2O and from H2O as the dihydrate. It also crystallises from CHCl3/Et2O as anhydrous crystals. The hydrate dehydrates at 120o/vacuum. Its solubility is 2.5% in CHCl3, 1.7% in EtOH, 0.25% in EtOAc, and 0.001% in H2O; and has E1cm 202.5 at 219-220nm (50% EtOH). [Stoll et al. Helv Chim Acta 37 1134 1954, Demoen & Janssen J Am Pharm Assoc 42 635 1953, Beilstein 18 IV 1478.]
ジギトキシン 上流と下流の製品情報
原材料
Dry acetone
アミルエーテル
ビス酢酸鉛(II)
ジヒドリド硫黄
D-ribo-Hex-1-enitol, 1,5-anhydro-2,6-dideoxy-4-O-[2,6-dideoxy-3,4-bis-O-[(1,1-dimethylethyl)dimethylsilyl]-β-D-ribo-hexopyranosyl]-3-O-[(1,1-dimethylethyl)dimethylsilyl]-
5-Hexyne-2,3-diol, 4-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-, 2-benzoate, (2R,3R,4S)-
D-ribo-Hex-1-enitol, 1,5-anhydro-2,6-dideoxy-3,4-bis-O-[(1,1-dimethylethyl)dimethylsilyl]-
準備製品