Tiotropium Bromide

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Chemical Structure| 136310-93-5 同义名 : BA679 BR; Tiotropium (bromide)
CAS号 : 136310-93-5
货号 : A166270
分子式 : C19H22BrNO4S2
纯度 : 98%
分子量 : 472.42
MDL号 : MFCD00867027
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Tiotropium bromide, a new long-lasting anticholinergic drug, binds with high affinity to muscarinic receptors but dissociates very slowly from M(1)- and M(3)-muscarinic receptors. Tiotropium bromide will become the most widely used bronchodilator for COPD (chronic obstructive pulmonary disease) patients in the future[3]. Moreover, Tiotropium inhalation attenuates RB-induced (Resistive breathing) pulmonary inflammation[4]. Tiotropium bromide at >15 pg/mL inhibited IL-8 production from both BEAS-2B cells and LFs (lung fibroblasts) after LPS stimulation, and thus may contribute to lower cellular inflammation in COPD[5].
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
NCT01257230 Asthma Phase 3 Completed - -
NCT02039011 Asthma Phase 4 Completed - United Kingdom ... 展开 >> Asthma and Allergy Research Group, University of Dundee Dundee, United Kingdom, DD1 3AU 收起 <<
NCT00949975 Chronic Obstructive Pulmonary ... 展开 >>Disease 收起 << Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL

参考文献

[1]Brandt C, Thronicke A, et al. Impact of Long-Term Tiotropium Bromide Therapy on Annual Lung Function Decline in Adult Patients with Cystic Fibrosis. PLoS One. 2016 Jun 28;11(6):e0158193.

[2]Barnes PJ, Belvisi MG, Mak JC, Haddad EB, O'Connor B. Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airways disease. Life Sci. 1995;56(11-12):853-9.

[3]Barnes PJ. Tiotropium bromide. Expert Opin Investig Drugs. 2001 Apr;10(4):733-40. doi: 10.1517/13543784.10.4.733. PMID: 11281822.

[4]Toumpanakis D, Loverdos K, Tzouda V, Vassilakopoulou V, Litsiou E, Magkou C, Karavana V, Pieper M, Vassilakopoulos T. Tiotropium bromide exerts anti-inflammatory effects during resistive breathing, an experimental model of severe airway obstruction. Int J Chron Obstruct Pulmon Dis. 2017 Jul 28;12:2207-2220. doi: 10.2147/COPD.S137587. PMID: 28814849; PMCID: PMC5546183.

[5]Suzaki I, Asano K, Shikama Y, Hamasaki T, Kanei A, Suzaki H. Suppression of IL-8 production from airway cells by tiotropium bromide in vitro. Int J Chron Obstruct Pulmon Dis. 2011;6:439-48. doi: 10.2147/COPD.S23695. Epub 2011 Sep 6. PMID: 22003289; PMCID: PMC3186742.