relaspium
Trospium chloride
CAS: 10405-02-4
Molecular Formula: C25H30ClNO3
relaspium - Names and Identifiers
relaspium - Physico-chemical Properties
| Molecular Formula | C25H30ClNO3 |
| Molar Mass | 427.96 |
| Melting Point | 266-268°C |
| Solubility | Very soluble in water, freely soluble in methanol, practically insoluble in methylene chloride. |
| Appearance | neat |
| Color | White to Off-White |
| Merck | 14,9786 |
| Storage Condition | Inert atmosphere,2-8°C |
relaspium - Risk and Safety
| RTECS | WH1424000 |
| HS Code | 2939800000 |
| Toxicity | Soly in water: ~1 g/2 ml. LD50 in mice (mg/kg): 12.3 i.v. (Antweiler) |
relaspium - Reference Information
| Antagonist | Trusonium chloride is an orally available quaternary ammonium compound with antagonistic muscarinic effects, also known as Tospim, whose chemical name is 3 -2-diphenylethanolyloxy spiro chloride (norscopolane -8,1 '-pyrrolidine, is a muscarinic antagonist developed by Rottapharm Madans, Italy, it was first marketed in Germany in 1990 and is widely used clinically as an anti-urinary incontinence drug. |
| biological activity | troxonium chloride is an orally active, specific and competitive muscarinic cholinergic receptor (mAChRs) antagonist with antimuscarinic activity. It can bind muscarinic receptors M1, M2 and M3 with high affinity, but does not bind to nicotinic and cholinergic receptors. |
| Target | Value |
| AChR | |
| indications | troxonium chloride is used to treat frequent urination, urgency and urge urinary incontinence caused by detrusor instability or detrusor hyperreflexia. |
| Pharmacological effects | The trastonium chloride is a synthetic tropine acid derivative with four ammonium groups. It is a parasympathetic nerve blocker and its effect is similar to atropine. It mainly works by competitively binding with the endogenous neurotransmitter acetylcholine to the postsynaptic membrane M receptor, it plays a role in reducing parasympathetic tension and removing smooth muscle spasm caused by parasympathetic nerves in organs innervated by parasympathetic nerves. It also has a certain effect on gastrointestinal, biliary tract and urinary tract. This product has low fat solubility and is not easy to pass through the blood-brain barrier, and will not produce side effects of the central nervous system. |
| drug interaction | 1. Strengthen the anticholinergic effects of drugs, such as amantadine, tricyclic antidepressants, quinidine, antihistamine and verapamil; Strengthen the cardiac acceleration effect of sympathomimetic drugs; Reduce the positive dynamic effects of drugs such as metoclopramide and cisapride. 2. Since this product can affect the motility and secretion of the gastrointestinal tract, it cannot be ruled out that this product will affect the absorption of other drugs taken at the same time. 3. since guar gum, cholestolamine and other drugs can not be ruled out to inhibit the absorption of this product, it is not recommended to use these drugs together with this product. 4. in vitro tests show that this product can affect the metabolism of cytochrome enzyme P450 (CYP1A2, 2A6, 2C9, 2C19, 2D19, 2D6, 2E1, 3A4) related to drug metabolism. It has no effect on other metabolism. |
| preparation | using tropin alcohol as raw material, through acylation and hydrolysis to generate despicin alcohol, despicin alcohol reacts with 1,4-dichlorobutane to generate chlorination (3q-despicin alcohol)- 8-spiro -1 '-pyrrolidinium salt, and then reacts with diphenylglycolic acid activated amide under the catalysis of DMAP to generate trisonium chloride. |
Last Update：2024-04-10 22:29:15
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