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132112-35-7

中文名称 盐酸罗哌卡因
英文名称 Ropivacaine hydrochloride
CAS 132112-35-7
分子式 C17H27ClN2O
MDL 编号 MFCD02102164
分子量 310.86
MOL 文件 132112-35-7.mol
更新日期 2024/03/28 15:14:07
132112-35-7 结构式 132112-35-7 结构式

基本信息

中文别名
盐酸罗哌卡因一水合物
(S)-1-丙基-2',6'-二甲基苯胺甲酰基哌啶单盐酸盐一水合物
(s)-罗哌卡因盐酸盐
(-)-S)-N-(2,6-二甲基苯基)-1-正丙基哌啶-2-甲酰胺盐酸盐
盐酸罗哌卡因
英文别名
ROPIVACAINE HCL
ROPIVACAINE HYDROCHLORIDE
ROPIVACAINE HYDROCHLORIDE MONOHYDRATE
ROPIVCACAINE HYDROCHLORIDE
S-ROPIVACAINE HCL
(S)-ROPIVACAINE HYDROCHLORIDE
(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
所属类别
原料药:局部麻醉剂

物理化学性质

熔点267-269°C
比旋光度D20 -7.28° (c = 2 in water)
储存条件2-8°C
溶解度H2O:可溶5mg/mL,澄清
形态粉末
颜色白色至灰白色
旋光性 (optical activity)[α]/D -9 to -12, c = 1 in methanol
InChIKeyVSHFRHVKMYGBJL-CKUXDGONSA-N

安全数据

危险性符号(GHS)
GHS05
警示词危险
危险性描述H318
危险品标志T,Xi
危险类别码26/27/28-41
危险品运输编号UN 2811 6.1 / PGIII
WGK Germany3
海关编码2933399090

常见问题列表

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
副作用

盐酸罗哌卡因的一般副作用有低血压、恶心、心动过缓、焦虑、感觉减退。

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 cell's 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 ).
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