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【Medlife小分子化合物专家】Ropivacaine HCl

2024年04月01日 13:45   生物.医药.天然产物  

上海陌孚医药科技有限公司 发布 访问商铺

关键词:Ropivacaine HCl

钠通道抑制剂。Ropivacaine hydrochloride 是 K2P (双孔钾通道) TREK-1 的抑制剂, 其 IC50 值为 402.7 μM。

中文名称    :Ropivacaine HCl
中文别名    :盐酸罗哌卡因;(-)-S)-N-(2,6-二甲基苯基)-1-正丙基***-2-甲酰胺盐酸盐;(s)-罗哌卡因盐酸盐;(S)-1-丙基-2',6'-二甲基苯胺甲酰基***单盐酸盐一水合物;N-(2,6-二甲基苯基)-1-正丙基***-2-甲酰胺盐酸盐;盐酸罗哌卡因,M.O.H.Standard In-house Standard;罗哌卡因(盐酸或甲磺盐)
英文名称    :Ropivacaine HCl
英文别名    :(S)-N-(2,6-Dimethylphenyl)-1-propylpiperidine-2-carboxamide hydrochloride;(S)-Ropivacaine Hcl;(S)-1-propyl-2',6'-dimethylanilinoformoxylpiperidine,monohydrochloride,monohydrate;Ropivacaine Hy drochloride;N-(2,6-Dimethylphenyl)-1-propyl-piperidine-2-carboxamide hydrochloride;Ropivacoine HCl anhydrous;2-Piperidinecarboxamide hydrochloride;ROPIVACAINE HCL;(2S)-N-(2,6-dimethylphenyl)-1-propyl-pipecolinamide hydrochloride;(S)-(-)-1-propyl-2',6'-pipecoloxylidide hydrochloride;(S)ROPIVACAINE HCL;PIPERIDINE-2-CARBOXAMIDE HYDROCHLORIDE API;REACTIVE YELLOW 145;ROPIVACAINE;ROPIVACAINE 1-HYDRATE;Ropivacaine hydrochl;ROPIVCACAINE HYDROCHLORIDE;S-ROPIVACAINE HCL;Ropivacaine hydrochloride;Naropin;Ropivacaine monohydrochloride;Ropivacaine hydrochloride hydrate;35504LBE2T;DSSTox_CID_28353;DSSTox_RID_82753;DSSTox_GSID_48379;(S)-Ropivacaine hydrochloride;2-Piperidinecarboxamide, N-(2,6-dimethylphenyl)-1-propyl-, monohydrochloride, (S)-;(S)-ropivacaine hydrochloride (anhydrous);C17H26N2O.HC
Cas No.    :98717-15-8
分子式    :C17H27ClN2O
分子量    :310.86
包装储存    :4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性    
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cells membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
性状    
Solid
IC50 & Target[1][2]    
IC50: sodium ion influx
IC50: 402.7 μM (TREK-1 in COS-7 cells membrane)
体内研究(In Vivo)    
Epidural administration of Ropivacaine hydrochloride effectively blocks neuropathic pain (both mechanical allodynia and heat hyperalgesia) without induction of analgesic tolerance and significantly delays the development of neuropathic pain produced by peripheral nerve injury.
Ropivacaine hydrochloride inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC).
Ropivacaine hydrochloride prevents pressure-induced lung edema and associated hyperpermeability as evidence by maintaining PaO2, lung wet-to-dry ratio and plasma volume in levels similar to sham rats.
Ropivacaine hydrochloride inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:    Adult Sprague-Dawley rats (300–400g)
Dosage:    1 μM
Administration:    Infusion (added to the perfusate reservoir)
Result:    Attenuated pressure-dependent increases in filtration coefficient (Kf).
运输条件    
Room temperature or refrigerated transportation.
储存方式    
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial    
参考文献    
[1]. Dene Simpson, et al. Ropivacaine: a review of its use in regional anaesthesia and acute pain management. Drugs. 2005;65(18):2675-717.  [Information]
[2]. Li TF, et al. Epidural sustained release ropivacaine prolongs anti-allodynia and anti-hyperalgesia in developing and established neuropathic pain. PLoS One. 2015 Jan 24;10(1):e0117321.  [Information]
[3]. Hye Won Shin, et al. The inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on K2P (two-pore domain potassium) channel TREK-1. J Anesth. 2014 Feb;28(1):81-6.  [Information]
[4]. Milan Patel, et al. Ropivacaine Inhibits Pressure-Induced Lung Endothelial Hyperpermeability in Models of Acute Hypertension. Life Sci. 2019 Apr 1;222:22-28.  [Information]

引用地址:https://www.med-life.cn/

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化工词典
  • 中文名称: 盐酸罗哌卡因
  • 英文名称: 2-Piperidinecarboxamide hydrochloride
  • CAS NO.: 98717-15-8
  • 分子式: C17H27ClN2O
  • 分子量:310.8621
盐酸罗哌卡因结构式图片|98717-15-8结构式图片
查看更多物化属性、结构等信息,点击: 98717-15-8
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