product name Tiotropium Bromide hydrate
Description: Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (also known as Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist. It is a long-acting bronchodilator that is used in the management of chronic obstructive pulmonary disease (COPD). Although it does not exhibit selectivity for specific muscarinic receptors, when topically applied it acts mainly on M3 muscarinic receptors located on smooth muscle cells and submucosal glands.
References: Respir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75.
490.43
Formula
C19H22NO4S2.Br.xH2O
CAS No.
139404-48-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 8 mg/mL (16.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BA 679BR
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390093
| In Vitro |
In vitro activity: 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). Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. Tiotropium bromide inhibits the Th2 cytokine production from PBMCs. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Respir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75. |
Related Posts
product name Tiotropium Bromide hydrate
Description: Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (also known as Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist. It is a long-acting bronchodilator that is used in the management of chronic obstructive pulmonary disease (COPD). Although it does not exhibit selectivity for specific muscarinic receptors, when topically applied it acts mainly on M3 muscarinic receptors located on smooth muscle cells and submucosal glands.
References: Respir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75.
490.43
Formula
C19H22NO4S2.Br.xH2O
CAS No.
139404-48-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 8 mg/mL (16.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BA 679BR
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19390093
| In Vitro |
In vitro activity: 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). Tiotropium significantly inhibits the release of chemotactic substances by AM, MonoMac6 and A549 cells. Tiotropium bromide inhibits the Th2 cytokine production from PBMCs. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. Tiotropium inhibits the increase in airway smooth muscle mass, myosin expression, and contractility in a guinea pig model of ongoing allergic asthma. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Respir Med. 2007 Nov;101(11):2386-94; Clin Exp Allergy. 2010 Aug;40(8):1266-75. |