中文同义词:
N-(2,6-二甲基苯基)-1-甲基-2-哌啶甲酰胺盐酸盐;盐酸甲哌卡因;盐酸卡波卡因;盐酸甲哌卡因?, BR;甲哌卡因杂质B;盐酸甲哌卡因, 局部麻醉, 电压门控NA+通道阻滞剂;甲哌卡因盐酸盐;盐酸甲哌卡因(碱基)
英文名称:
Mepivacaine hydrochloride
英文同义词:
Mepivacaine Hydrochloride (200 mg);Ropivacaine base Mepivacaine HCL;(1-methyl-dl-piperidine-2-carboxylicacid)-2,6-dimethylanilidehydrochloride;1-methyl-2’,6’-pipecoloxylididehydrochloride;Mepivacaine HCl USP;2-Piperidinecarboxamide, N-(2,6-dimethylphenyl)-1-methyl-, monohydrochloride;2,6-Pipecoloxylidide, 1-methyl-, monohydrochloride (6CI, 8CI);2-Piperidinecarboxamide, N-(2,6-dimethylphenyl)-1-methyl-, monohydrochloride (9CI)
相关类别:
医药原料;局部麻醉系列;麻醉类;小分子抑制剂;原料药;对照品-杂质对照品;麻醉药及其辅助药物;药物杂质及中间体;医药原料药;Sodium channel;Amines;Aromatics;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;Analgesic series;API
溶解度
H2O: soluble20mg/mL, clear
CAS 数据库
1722-62-9(CAS DataBase Reference)
EPA化学物质信息
2-Piperidinecarboxamide, N-(2,6-dimethylphenyl)-1-methyl-, monohydrochloride (1722-62-9)
生物活性
Mepivacaine 是一种叔胺,用作局部麻醉剂。
体外研究
Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization. This leads to a blockage of nerve impulse initiation and conduction and results in a reversible loss of sensation. Compared to other local anesthetics, this agent has a more rapid onset and moderate duration of action.
Mepivacaine hydrochloride has a reasonably rapid onset (more rapid than that of procaine) and medium duration of action (shorter than that of procaine).
Mepivacaine hydrochloride displays a preferential use-dependent block of Na(v)1.8, S(-)-bupivacaine displays a preference for TTXs Na(+) channels.
体内研究
对马的测试表明,与根据以前解剖的,乳胶注射后得到的假定相比,mepivacaine在相邻关节结构间具有更大的扩撒,与关节造影研究形成对比。经历膝关节镜检查患者中,与神经刺激相比较,超声处理使1.5% mepivacaine阻断坐骨神经所需的最低有效麻醉剂体积(MEAV50)减少37%。在犬齿和前臼齿中,lidocaine制剂与肾上腺素相比,3%mepivacaine的使用使麻醉时间间隔更短。
急性毒性
腹腔-小鼠 LD50: 117 毫克/公斤; 静脉-小鼠 LD50: 35 毫克/公斤
危险品运输编号
UN 2811 6.1 / PGIII
毒性
LD50 in mice, rats (mg/kg): 280, 500 s.c. (Aberg)