132112-35-7
132112-35-7 结构式
基本信息
(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
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
物理化学性质
制备方法
84057-95-4
132112-35-7
以(S)-N-(2,6-二甲基苯基)-1-丙基-2-哌啶羧酰胺为原料，合成(S)-N-(2,6-二甲基苯基)-1-丙基哌啶-2-甲酰胺盐酸盐水合物的一般步骤如下：将约3g (S)-N-(2,6-二甲基苯基)-1-丙基-2-哌啶羧酰胺溶于10mL去离子水中，向该溶液中缓慢加入50mL预热至60°C的丙酮。在搅拌条件下，逐滴加入浓盐酸，调节pH至2.0。随后，将反应混合物加热至回流，直至形成澄清溶液。向反应体系中追加20mL丙酮，冷却至室温后过滤析出的固体产物。用冷丙酮洗涤固体三次，于40°C真空干燥箱中干燥12小时，得到白色结晶状(S)-N-(2,6-二甲基苯基)-1-丙基哌啶-2-甲酰胺盐酸盐水合物2.9g，产率82%。经卡尔费休法测定，产物水含量为5.6%。
参考文献：
[1] Patent: US2006/276654, 2006, A1. Location in patent: Page/Page column 5
[2] Patent: US2006/276654, 2006, A1. Location in patent: Page/Page column 5
常见问题列表
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
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。
IC50: sodium ion influxIC50: 402.7 μM (TREK-1 in COS-7 cell's membrane)
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。
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 ). |