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Diphenidol HCl

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Chemical Structure| 3254-89-5 同义名 : Difenidol hydrochloride;Diphenidol (hydrochloride);SKF 478A;Diphenidol hydrochloride
CAS号 : 3254-89-5
货号 : A191183
分子式 : C21H28ClNO
纯度 : 98%
分子量 : 345.906
MDL号 : MFCD00151479
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: 45 mg/mL(130.09 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

H2O: 15 mg/mL(43.36 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • mAChR
描述 Diphenidol hydrochloride is a muscarinic antagonist employed as an antiemetic and as an antivertigo agent. Diphenidol exhibited a concentration- and state-dependent effect on tonic blockade of voltage-gated Na+ currents in mouse neuroblastoma N2A cells (IC50 of 0.77 and 62.6 mM at holding potentials of -70 and -100 mV, respectively)[3]. Diphenidol has been shown to block voltage-gated Na+ channels, which are associated with specific types of pain.Systemic diphenidol produced a dose-related inhibition of mechanical allodynia following chronic constriction injury of the sciatic nerve[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
NCT01574313 Vertigo Menie... 展开 >>re Disease 收起 << Phase 4 Completed - Taiwan ... 展开 >> i Mei Medical Center Tainan, Taiwan, Taiwan Tainan, Taiwan, 70014 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.45mL

2.89mL

1.45mL

28.91mL

5.78mL

2.89mL
参考文献

[1]Leung YM, Wong KL, et al. Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol. Pharmacol Rep. 2012;64(3):739-44.

[2]Leung YM, Wu BT, Chen YC, Hung CH, Chen YW. Diphenidol inhibited sodium currents and produced spinal anesthesia. Neuropharmacology. 2010 Jun;58(7):1147-52.

[3]Leung YM, Wu BT, Chen YC, Hung CH, Chen YW. Diphenidol inhibited sodium currents and produced spinal anesthesia. Neuropharmacology. 2010 Jun;58(7):1147-52. doi: 10.1016/j.neuropharm.2010.02.007. Epub 2010 Feb 20.

[4]Chen YW, Tzeng JI, Liu KS, Yu SH, Hung CH, Wang JJ. Systemic diphenidol reduces neuropathic allodynia and TNF-alpha overexpression in rats after chronic constriction injury. Neurosci Lett. 2013 Sep 27;552:62-5.