Trospium chloride 是一种具有口服活性、特异性和竞争性的毒蕈碱胆碱能受体 (mAChRs) 拮抗剂，具有抗毒蕈碱活性。
| Cas No. | 10405-02-4 |
| 别名 | 曲司氯铵 |
| 化学名 | [(1R,5S)-spiro[8-azoniabicyclo[3.2.1]octane-8,1'-azolidin-1-ium]-3-yl] 2-hydroxy-2,2-diphenylacetate;chloride |
| Canonical SMILES | C1CC[N+]2(C1)C3CCC2CC(C3)OC(=O)C(C4=CC=CC=C4)(C5=CC=CC=C5)O.[Cl-] |
| 分子式 | C25H30NO3.Cl |
| 分子量 | 427.96 |
| 溶解度 | ≥ 21.4mg/mL in DMSO |
| 储存条件 | Store at 2-8℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Trospium Chloride is a competitive muscarinic cholinergic receptor antagonist.Target: mAChRTrospium chloride is an antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Trospium has pharmacologic properties that are distinct from other antimuscarinic agents [1]. After oral administration, absorption of the hydrophilic trospium chloride is slow and incomplete. Peak plasma concentrations (Cmax) of approximately 4 ng/mL are reached 4-5 hours after administration of a 20 mg immediate-release preparation. The mean bioavailability is approximately 10% and decreases by concomitant food intake (to a mean of 26% of the fasting area under the plasma concentration-time curve [AUC]). Trospium chloride displays dose proportional increases in AUC and Cmax after a single dose within the clinically relevant dose range (20-60 mg). The mean volume of distribution is approximately 350-800 L [2]. References:
[1]. Staskin, D.R., Trospium chloride: Distinct among other anticholinergic agents available for the treatment of overactive bladder. Urol Clin North Am, 2006. 33(4): p. 465-73, viii.
[2]. Doroshyenko, O., et al., Clinical pharmacokinetics of trospium chloride. Clin Pharmacokinet, 2005. 44(7): p. 701-20. |
