噻托溴铵一水合物 T6707

Product Introduction
Bioactivity


英文名: Tiotropium Bromide hydrate

描述: Tiotropium Bromide hydrate (BA-679 BR hydrate) 是长效的毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性气道疾病 (COPD)。

体外活性: Tiotropium bromide is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. Tiotropium bromide has a potent inhibitory effect against cholinergic nerve-induced contraction of guinea-pig and human airways, that has a slower onset than atropine or ipratropium bromide. Tiotropium bromide, ipratropium bromide and atropine all increase ACh release on neural stimulation and that this effect is washed out equally quickly for the three antagonists. Tiotropium bromide dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals). [1] Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. [2] Tiotropium bromide inhibits the Th2 cytokine production from PBMCs. [3]

体内活性: Tiotropium bromide significantly reduces airway inflammation and the Th2 cytokine production in bronchoalveolar lavage fluid (BALF) in both acute and chronic mouse models of asthma. Tiotropium bromide significantly decreases the goblet cell metaplasia, thickness of airway smooth muscle, and airway fibrosis in a mouse model of asthma. Tiotropium bromide reduces the levels of TGF-beta1 in BALF in a chronic model. [3] Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. [4] Tiotropium abrogates the LPS-induced increase in neutrophils, goblet cells, collagen deposition and muscularised microvessels in a guinea pig model of chronic obstructive pulmonary disease (COPD), but has no effect on emphysema. [5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 8 mg/mL (16.31 mM)


关键字: Tiotropium Bromide hydrate | BA-679 BR Hydrate | Tiotropium Bromide Hydrate

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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Macrocyclic Compound Library | Bioactive Compounds Library Max | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途