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Pentoxyverine citrate

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Chemical Structure| 23142-01-0 同义名 : 枸橼酸喷托维林 ;Carbetapentane citrate;Carbetapentane (citrate);Loucarbate;Pentoxiverine citrate
CAS号 : 23142-01-0
货号 : A363600
分子式 : C26H39NO10
纯度 : 98%
分子量 : 525.589
MDL号 : MFCD00055697
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(66.59 mM)，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
动物实验配方：
生物活性
靶点

  • mAChR
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 - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.51mL

1.90mL

0.95mL

19.03mL

3.81mL

1.90mL
参考文献

[1]Donmez OA, Asci B, et al. Simultaneous determination of potassium guaiacolsulfonate, guaifenesin, diphenhydramine HCl and carbetapentane citrate in syrups by using HPLC-DAD coupled with partial least squares multivariate calibration. Talanta. 2011 Feb 15;83(5):1601-5.

[2]Brown C, Fezoui M, et al. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004 Jan;141(2):233-40.

[3]Abo Dena AS, Ali AM, El-Sherbiny IM. Carbetapentane citrate. Profiles Drug Subst Excip Relat Methodol. 2020;45:41‐53

[4]Leung YM, Tzeng JI, Kuo CS, Chen YW, Chu CC, Wang JJ. The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents. Eur J Pharmacol. 2013;714(1-3):366‐372

[5]Leander JD. Evaluation of dextromethorphan and carbetapentane as anticonvulsants and N-methyl-D-aspartic acid antagonists in mice. Epilepsy Res. 1989;4(1):28‐33

[6]Kim HC, Jhoo WK, Kim WK, et al. Carbetapentane attenuates kainate-induced seizures via sigma-1 receptor modulation. Life Sci. 2001;69(8):915‐922