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Trospium chloride

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Chemical Structure| 10405-02-4 同义名 : 曲司氯胺 ;Trospium (chloride);Relaspium
CAS号 : 10405-02-4
货号 : A293957
分子式 : C25H30ClNO3
纯度 : 99%
分子量 : 427.964
MDL号 : MFCD00865254
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(81.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(233.66 mM)
动物实验配方：
生物活性
靶点

  • AChR
描述 Trospium Chloride is antagonist of acetylcholine muscarinic receptors and the cornerstone of pharmacotherapy for the symptoms of overactive bladder (OAB). Trospium chloride, dosed 20 mg twice daily, is significantly superior to placebo in improving cystometric parameters, reducing urinary frequency, reducing incontinence episodes, and increasing urine volume per micturition[3]. Moreover, trospium chloride (1 mg/kg, intravenously) permeation across the BBB (blood-brain barrier ) is not increased in ageing perse, and therefore, the occurrence of adverse CNS (central nervous system) drug effects is also not expected to increase with ageing[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02386072 - Completed - -
NCT00547378 Urinary Incontinence, Urgency-... 展开 >>frequency Overactive Bladder 收起 << Phase 4 Completed - -
NCT01499069 Overactive Bladder Not Applicable Unknown December 2015 Korea, Republic of ... 展开 >> Samsung Medical Center Recruiting Seoul, Korea, Republic of, 135-710 Contact: Kyu-Sung Lee, Ph.D    82-2-3410-3554    ksleedr@skku.edu    Contact: Bong-Hee Lim, BA    82-2-3410-3743    bonghee.lim@sbri.co.kr    Sub-Investigator: Deok Hyun Han, PhD          Sub-Investigator: Young-Suk Lee, PhD          Sub-Investigator: Ha Na Lee, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.68mL

2.34mL

1.17mL

23.37mL

4.67mL

2.34mL
参考文献

[1]Staskin DR. Trospium chloride: Distinct among other anticholinergic agents available for the treatment of overactive bladder. Urol Clin North Am. 2006 Nov;33(4):465-73, viii.

[2]Doroshyenko O, Jetter A, et al. Clinical pharmacokinetics of trospium chloride. Clin Pharmacokinet. 2005;44(7):701-20.

[3]Guay DR. Trospium chloride: an update on a quaternary anticholinergic for treatment of urge urinary incontinence. Ther Clin Risk Manag. 2005 Jun;1(2):157-67. doi: 10.2147/tcrm.1.2.157.62912. PMID: 18360555; PMCID: PMC1661617.

[4]Kranz J, Petzinger E, Geyer J. Brain penetration of the OAB drug trospium chloride is not increased in aged mice. World J Urol. 2013 Feb;31(1):219-24. doi: 10.1007/s00345-011-0803-z. Epub 2011 Nov 27. PMID: 22120415; PMCID: PMC3557395.