盐酸罗哌卡因

概述用途副作用生物活性靶点体外研究体内研究盐酸罗哌卡因试剂级价格

盐酸罗哌卡因

CAS号:132112-35-7
英文名:Ropivacaine hydrochloride
中文名:盐酸罗哌卡因
CBNumber:CB0369811
分子式:C17H26N2O.ClH.H2O
分子量:328.88
MOL File:132112-35-7.mol

盐酸罗哌卡因化学性质

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: 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)

安全信息

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

盐酸罗哌卡因性质、用途与生产工艺

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 ).