盐酸罗哌卡因

中文名称:

盐酸罗哌卡因

中文同义词:

盐酸罗哌卡因(标准品);单水罗哌卡因盐酸盐;盐酸罗哌卡因一水物;罗哌卡因 盐酸水;盐酸罗哌卡因(碱基);ROPIVACAINE HCL 盐酸罗哌卡因;盐酸罗哌卡因对照品;盐酸罗哌卡因一水合物

英文名称:

Ropivacaine hydrochloride

英文同义词:

(S)-1-propyl-2,6-dimethylanilinoformoxylpiperidine monohydrochloride monohydrate;(S)-1-propyl-2,6-dimethylanilinoformoxylpiperidine,monohydrochloride,monohydrate;(S)-Ropivaxaine hydrochloride;(S)-N-(2,6-dimethylphenyl)-1-propylpiperidine-2-carboxamide hydrochloride;Ropivacaine hydrochloride;(2S)-N-(2,6-Dimethylphenyl)-1-propyl-2-piperidinecarboxamide Hydrochloride Hydrate;LEA-103;(S)-ropivacaine hydrochloride hydrate

CAS号:

132112-35-7

分子式:

C17H26N2O.ClH.H2O

分子量:

328.88

EINECS号:

663-286-1

相关类别:

有机化工中间体;医药原料药-科研原料;麻醉剂类Narcotic;原料药;局部麻醉系列;中间体;其他科研原料药;医药原料;合成;小分子抑制剂，天然产物;酰胺类局麻药;Chiral Reagents;Intermediates Fine Chemicals;Pharmaceuticals;麻醉类;Inhibitors;API;医药原料和中间体;中间体类;原料;贝尔卡主打

Mol文件:

132112-35-7.mol

熔点 

267-269°C

比旋光度 

D20 -7.28° (c = 2 in water)

储存条件 

Refrigerator

溶解度 

H2O: soluble5mg/mL, clear

形态

powder

颜色

white to off-white

旋光性 (optical activity)

[α]/D -9 to -12, c = 1 in methanol

InChIKey

VSHFRHVKMYGBJL-CKUXDGONSA-N

CAS 数据库

132112-35-7(CAS DataBase Reference)

概述

盐酸罗哌卡因为酰胺类长效局麻药。其脂溶性大于利多卡因，小于布比卡因，其麻醉强度为普鲁卡因的8倍。因其在肝脏代谢的产物也有局麻作用，故作用较持久。主要用于区域阻滞麻醉和硬膜外麻醉，用于术后和分娩的镇痛。

用途

盐酸罗哌卡因适用于: 外科手术麻醉 -----硬膜外麻醉，包括剖宫产术 -----蛛网膜下腔麻醉 -----区域阻滞 急性疼痛控制 -----持续硬膜外输注或间歇性单次用药，如术后或阴道分娩镇痛 -----区域阻滞

生物活性

Ropivacaine HCl (LEA-103) 是一种麻醉剂，通过可逆地抑制钠离子流入来阻断神经纤维上冲动的传导。

靶点

IC50: sodium ion influxIC50: 402.7 μM (TREK-1 in COS-7 cells membrane)

体外研究

Ropivacaine HCl是一种局部麻醉剂。Ropivacaine HCl通过可逆抑制神经纤维中钠离子流引起神经阻滞。Ropivacaine HCl的pKa是~8.2。Ropivacaine HCl在高血浆浓度下具有诱导心血管毒性和CNS毒性的可能性。

体内研究

Epidural administration of Ropivacaine hydrochloride monohydrate 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 monohydrate inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC). Ropivacaine hydrochloride monohydrate 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 monohydrate inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs. 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 (K f ).

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 (K f ).

危险品标志 

T,Xi

危险类别码 

26/27/28-41

安全说明 

22-36/37/39-45-39-26

危险品运输编号 

UN 2811 6.1 / PGIII

WGK Germany 

3

海关编码 

2933399090