Molecular Formula | C19H22BrNO4S2.H2O |
Molar Mass | 490.43 |
Solubility | Sparingly soluble in water, soluble in methanol, practically insoluble in methylene chloride. |
In vitro study | In the airways of guinea pigs and humans, Tiotropium bromide has an anticholinergic nerve-induced contraction with a slower onset of action than atropine or ipratropium bromide. Tiotropium bromide, ipratropium bromide and atropine all increase the release of neurostimulatory acetylcholine, and the effect of this triple antagonist is washed away equally rapidly. The Tiotropium bromide dissociates slowly from the M3 receptor (upper airway smooth muscle) and rapidly from the M2 self-receptor (cholinergic nerve terminals). Tiotropium bromide significantly inhibited the release of chemotactic substances from AM,MonoMac6 and A549 cells. Tiotropium bromide inhibits the production of Th2 type cytokines from PBMC. |
In vivo study | In mouse models of acute and chronic asthma, Tiotropium bromide significantly reduces airway inflammation and th2-type cytokine production in bronchoalveolar lavage fluid (BALF). In a mouse model of asthma, Tiotropium bromide significantly reduced goblet cell transformation, airway smooth muscle thickness, and airway fibrosis. Tiotropium bromide reduces transforming growth factor-β1 levels in bronchoalveolar lavage fluid in a chronic model. In a guinea pig model of allergic asthma, Tiotropium bromide inhibits myosin expression in increasing airway smooth muscle mass, and contraction. In a guinea pig model of chronic obstructive pulmonary disease (COPD), Tiotropium bromide abrogated LPS-induced increases in neutrophils, goblet cells, collagen deposition, and muscularised microvessels, but had no effect on emphysema. |
biological activity | Tiotropium Bromide hydrate (BA 679BR) is a monohydrate of Tiotropium bromide (Spiriva; Tiova; BA 679BR; Tiopropium), which is an anticholinergic, bronchodilator and muscarinic receptor antagonist. |
Target | Value |