|2-(2-(二乙氨基)乙氧基)乙基 1-苯基环戊烷-1-羧酸酯 2-羟基丙烷-1,2,3-三羧酸盐|CsnPharm

CAS No.: 23142-01-0

咳必清 Catalog No. CSN10546

Synonyms: Pentoxyverine citrate;Carbetapentane (citrate);Pentoxiverine citrate

Carβpentane citrate is a selective inhibitor of mAchR with Ki value of 76nM, also binds to serotonin 5-HT3 with Ki value of 7.9 nM and works as an agonist of the sigma-1 receptor (Ki = 10.4 nM).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Carbetapentane citrate, a non-opioid centrally-acting antitussive drug, is a common treatment for cough associated with other diseases such as common cold and respiratory tract infections. Its mode of action is very close to that of atropine; since it acts at the level of the peripheral parasympathetic nerve endings. The drug reaches its maximum plasma concentration (Cmax) 2h after administration, and it has a plasma half-life of 2.3h in case of oral administration^[3]. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade. Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33 Hz), 50 µM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block^[4]. Carbetapentane had an anticonvulsant action without protecting against NMDA-induced lethality^[5]. Carbetapentane pretreatment also significantly attenuated the KA-induced (kainic acid) increase in Fos-related antigen immunoreactivity in the hippocampus. Carbetapentane provides neuroprotection against KA insult via sigma-1 receptor modulation^[6].
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
NCT02183649 Healthy Phase 1 Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02183649	Healthy	Phase 1	Completed	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9026 mL
- 9.5131 mL
- 19.0263 mL
- 5 mM
- 0.3805 mL
- 1.9026 mL
- 3.8053 mL
- 10 mM
- 0.1903 mL
- 0.9513 mL
- 1.9026 mL

技术信息

CAS号

23142-01-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H39NO10

运输

蓝冰

分子量

525.59

别名

Pentoxyverine citrate;Carbetapentane (citrate);Pentoxiverine citrate;Loucarbate;Carbetapentane Citrate;咳必清;枸橼酸喷托维林

溶解度

DMSO	98.0 mg/mL (186.5 mM)
Ethanol	8.0 mg/mL (15.2 mM)

动物实验配方

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