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CAS No.: 869113-09-7

芜地溴铵 Catalog No. CSN13851

Synonyms: GSK573719A;Umeclidinium (bromide);GSK-573719

Umeclidinium bromide is a long-acting mAchR antagonist with Ki values ranging in 0.05 to 0.16 nM for the cloned human M1-M5 mAChRs.

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生物活性

描述Activation of muscarinic subtype 3 (M3) muscarinic cholinergic receptors (mAChRs), which is highly expressed on the airway smooth muscle, increases airway tone, whereas its blockade improves lung function and quality of life in patients with pulmonary diseases. Umeclidinium Bromide is a novel mAChR antagonist with the affinity (K_i) for the cloned human M1-M5 mAChRs ranged from 0.05 to 0.16 nM. In cells containing the human recombinant M3 mAChR, the CRC (concentration-response curves) obtained with Ach was shifted rightward in the presence of Umeclidinium Bromide (1–1000 nM) in a concentration-dependent manner. Additional cellular studies showed that the effects of Umeclidinium Bromide on the M3 mAChR–mediated activity were slowly reversible. Pretreatment of CHO cells with Umeclidinium Bromide (3.3–330 nM for 30 minutes) produced rightward displacement of the Ach CRC comparable to that obtained previously. The changes in contractile activity were concentration-dependently blocked by preincubation (120 minutes) of the tissues with Umeclidinium Bromide (1–100 nM), thereby displacing the Cch-CRC to the right in a parallel manner. The time to 50% of maximal relaxation(termed ON t_1/2) for Umeclidinium Bromide was concentration-dependent and decreased in value as the concentration of antagonist was increased. When administered intranasally as a solution, Umeclidinium Bromide blocked nebulized methacholine (30 mg/ml or ED₈₀ value for maximal bronchoconstriction) in a dose-dependent manner (ED₅₀ = 0.02 μg per mouse measured 5 hours after instillation). Intratracheal instillation of Umeclidinium Bromide (0.25, 2.5, and 25 μg per guinea pig) dose dependently blocked the increase in Penh elicited by aerosolized Ach. At the highest dose of Ach (100 μg i.v.), significant inhibition, i.e., 74.4%, P＜0.05, was obtained 4 hours after instillation of 0.25 μg per guinea pig of Umeclidinium Bromide^[3].
参考文献

[1] Salmon M, Luttmann MA, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptorsfor treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70.
[2] Cazzola M, Page CP, et al. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012 Jul;64(3):450-504.
[3] Salmon M, Luttmann MA, Foley JJ, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013;345(2):260‐270

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9666 mL
- 9.8330 mL
- 19.6661 mL
- 5 mM
- 0.3933 mL
- 1.9666 mL
- 3.9332 mL
- 10 mM
- 0.1967 mL
- 0.9833 mL
- 1.9666 mL

技术信息

CAS号

869113-09-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H34BrNO2

运输

蓝冰

分子量

508.49

别名

GSK573719A;Umeclidinium (bromide);GSK-573719;Incruse Ellipta;芜地溴铵

溶解度

DMSO	140.0 mg/mL (275.3 mM)
Water	insoluble

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