ChemicalBook
Chinese english Germany Korea

チオトロピウムブロミド

チオトロピウムブロミド 化学構造式
136310-93-5
CAS番号.
136310-93-5
化学名:
チオトロピウムブロミド
别名:
チオトロピウムブロミド
英語化学名:
Tiotropium bromide
英語别名:
Ba-679;Ba-679 BR;TiopropiuM;otropiuM broMide;TIOTROPIUM BROMIDE;Tiotropium bromide, >=99%;Anhydrous Tiotropium Bromide;TiotropiuM broMide anhydrous;Tiotropium Bromide Impurity 8;TiotropiuM BroMide(Spiriva, BA 679BR)
CBNumber:
CB4244930
化学式:
C19H22BrNO4S2
分子量:
472.42
MOL File:
136310-93-5.mol

チオトロピウムブロミド 物理性質

融点 :
218-2200C
貯蔵温度 :
Refrigerator
極大吸収波長 (λmax):
240nm(lit.)
Merck :
14,9454
CAS データベース:
136310-93-5(CAS DataBase Reference)

安全性情報

チオトロピウムブロミド 価格 もっと(11)

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) W01CAY15773
Tiotropium (bromide)
136310-93-5 1mg ¥13600 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01CAY15773
Tiotropium (bromide)
136310-93-5 5mg ¥26500 2018-12-26 購入
東京化成工業 T3032 チオトロピウムブロミド >98.0%(HPLC)(T)
Tiotropium Bromide >98.0%(HPLC)(T)
136310-93-5 200mg ¥37000 2018-12-04 購入
東京化成工業 T3032 チオトロピウムブロミド >98.0%(HPLC)(T)
Tiotropium Bromide >98.0%(HPLC)(T)
136310-93-5 50mg ¥12400 2018-12-04 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-7472 チオトロピウムブロミド
Tiotropium bromide
136310-93-5 250mg ¥43200 2018-12-26 購入

チオトロピウムブロミド 化学特性,用途語,生産方法

説明

Tiotropium bromide is a long-acting inhaled muscarinic antagonist, developed for the once-daily treatment of chronic obstructive pulmonary disease. Tiotropium bromide can be prepared in three steps. The Grignard condensation of 2-thienyl magnesium bromide with oxalic acid dimethyl ester, followed by a transesterlfication with scopine provided the ester which was quaternized with methyl bromide. Tiotropium bromide binds to human recombinant muscarinic receptors M1-, M2- and M3-subtypes with high and similar affinity, comparable to those obtained with ipratropium. Tiotropium bromide is characterized by its novel property of kinetic selectivity : while ipratropium rapidly dissociated from each of the receptor subtypes, tiotropium dissociated rapidly from M2 receptors (t1/2=3.6 h) but slowly from MI (t1/2=14.6 h) and M3 (t1/2=34.7 h) receptors. Inhibition of cholinergic bronchospasm by tiotropium bromide was demonstrated in anesthetized guinea pigs, rabbits and dogs. In healthy volunteers, inhalation of tiotropium bromide resulted in an absolute bioavailability of 19.5%, a t,,, value of 5 min. and the terminal half-life value of 5-6 days. There was no evidence of drug accumulation after repeated administration. The extent of biotransfonation was small with a urinary excretion of 74% of unchanged substance after iv. administration. Long term studies in patients with stable COPD have demonstrated that tiotropium bromide gave an effective bronchodilation that was maintained over 24h, significantly improved lung function as measured by FEVI (+ll-12%) and showed progressive reduction in dyspnea. It also reduced exacerbations of COPD patients and improved quality of life. Tiotropium bromide produced greater and more sustained bronchodilation than ipratropium bromide. Tiotropium has been shown to cause superior bronchodilatation and symptomatic improvements when compared to twice daily salmeterol in COPD. Tiotropium bromide was well tolerated and caused few adverse effects. The most common side effect reported was the mechanism-related effect of dry mouth.

化学的特性

White Solid

Originator

Boehringer lngelheim (Germany)

使用

Muscarinic receptor antagonist. Bronchodilator

使用

Specially selective choline drug resistance

使用

Anti - Asthmatic

定義

ChEBI: An organic bromide salt having (1alpha,2beta,4beta,5alpha,7beta)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]non ne as the counterion. Used (in the form of the hydrate) for maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease.

brand name

Spiriva

一般的な説明

Tiotropium bromide, (1 ,2 ,4 ,7 )-7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane, (Spiriva) is anantimuscarinic agent that is used in an inhalation device to deliverthe drug into the lungs. It is indicated in the treatment ofchronic obstructive pulmonary disease (COPD), includingchronic bronchitis and emphysema. The standard once-dailydose is 18 g of tiotropium.

薬物動態学

Tiotropium is administered as a dry powder via inhalation using a HandiHaler, in which is placed the drug, contained in a green capsule. Patients should be cautioned not to be confused and take the medication orally. Systemic distribution following oral inhalation is minimal, essentially because of its hydrophilic character. If swallowed, only approximately 14% of the dose is eliminated in the urine, with the remainder being found in the feces. Inhaled tiotropium has a 30-minute onset of action but a much longer duration of action than ipratropium (24 versus <4 hours, respectively). Tiotropium is metabolized by both CYP3A4 and CYP2D6, followed by glutathione conjugation to a variety of metabolites. Only a very small amount is nonenzymatically hydrolyzed to inactive products.

臨床応用

Tiotropium is the dithienyl derivative of N-methyl scopolamine, a quaternary analogue of naturally occurring scopolamine in Atropa belladonna. It is indicated primarily for the relief of bronchospasms associated with COPD and can be considered to be a site-specific, local medication to the lung.

副作用

Tiotropium has an adverse reaction profile similar to that of ipratropium, with dry mouth being the most common adverse effect; however, blurred vision, tachycardia, urinary difficulty, headache precipitation, and exacerbation of narrow-angle glaucoma have been reported.

チオトロピウムブロミド 上流と下流の製品情報

原材料

準備製品


チオトロピウムブロミド 生産企業

Global( 262)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Anhui Dexinjia Biopharm Co., Ltd
86-531-82375818
86-531-82375893 alice@jndxj.com CHINA 165 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21837 58
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24754 60
Hebei Minshang Biotechnology Co., Ltd
+86-13582176207 +86-13582176207
cathy@hbminshang.cn CHINA 312 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30043 58
Hebei Huanhao Biotechnology Co., Ltd.
+8618034552304
86-0311-83975816 cathylee@hbhuanhao.com CHINA 865 58

136310-93-5(チオトロピウムブロミド)キーワード:


  • 136310-93-5
  • Tiotropium Bromide Impurity 8
  • (1α,2β,4β,5α,7β)-7-[(Hy-droxydi-2-thienylacetyl)axy]-9,9-dimethyl-3-oxa-9-azoniatri-cyclo[3.3.1.02.4]nonane
  • Anhydrous Tiotropium Bromide
  • (1R,2R,4S,5S,7s)-7-[(2-Hydroxy-2,2-dithiophen-2-ylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide monohydrate
  • Tiotropium Bromide cas136310-93-5(whatsapp:+8618830163278)
  • 3-Oxa-9-azoniatricyclo[3.3.1.02,4]nonane, 7-[(2-hydroxy-2,2-di-2-thienylacetyl)oxy]-9,9-dimethyl-, bromide (1:1), (1α,2β,4β,5α,7β)-
  • (1a,2,4,5a,7)-7-[(2-Hydroxy-2,2-di-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane Bromide
  • (1α,2β,4β,5α,7β-7-[(Hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0^<2,4>^]nonane bromide
  • Ba-679
  • Ba-679 BR
  • otropiuM broMide
  • TiotropiuM broMide anhydrous
  • (1R,2S,4R,5S,7R)-7-{[2-hydroxy-2,2-bis(thiophen-2-yl)acetyl]oxy}-9,9-diMethyl-3-oxa-9-azatricyclo[3.3.1.0^{2,4}]nonan-9-iuM broMide
  • TiotropiuM BroMide(Spiriva, BA 679BR)
  • (1α,2β,4β,5α,7β)-7-[(2-Hydroxy-2,2-di-2-thienylacetyl)oxy]-9,9-diMethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane BroMide
  • 3-Oxa-9-azoniatricyclo[3.3.1.02,4]nonane,7-[(2-hydroxy-2,2-di-2-thienylacetyl)oxy]-9,9-diMethyl-, broMide (1:1), (1a,2b,4b,5a,7b)-
  • TiopropiuM
  • (1R,2R,4S,5S,7s)-7-(2-Hydroxy-2,2-di(thiophen-2-yl)acetoxy)-9,9-diMethyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-9-iuM broMide
  • Tiotropium bromide, >=99%
  • TIOTROPIUM BROMIDE
  • (1a,2b,4b,5a,7b)-7-[(Hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide
  • チオトロピウムブロミド
Copyright 2017 © ChemicalBook. All rights reserved