Tiotropium Bromide 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)。

Tiotropium Bromide hydrate is an anticholinergic and bronchodilator. Tiotropium Bromide hydrate is also a muscarinic receptor antagonist. Target: mAChR Tiotropium bromide (Ba 679 BR) is a novel potent and long-lasting muscarinic antagonist that has been developed for the treatment of chronic obstructive airways disease (COPD). Binding studies with [3H]tiotropium bromide in human lung have confirmed that this is a potent muscarinic antagonist with equal affinity for M1-, M2- and M3-receptors and is approximately 10-fold more potent than ipratropium bromide. In vitro 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 dissociates slowly from M3-receptors (on airway smooth muscle) but rapidly from M2 autoreceptors (on cholinergic nerve terminals) [1]. Tiotropium bromide is a quaternary ammonium derivative that binds to muscarinic receptors. However, although tiotropium binds with high affinity to muscarinic receptors of M1-, M2- and M3-subtypes, it dissociates very slowly from M1- and M3-receptors but more rapidly from M2-receptors, thereby giving it a unique kinetic selectivity [2].

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]

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]

411207-31-3

C19H24BrNO5S2

490.43

BA-679 BR hydrate;BA 679BR;噻托溴铵一水合物

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:8 mg/mL (16.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years