盐酸甲哌卡因 T0946

Product Introduction
Bioactivity


英文名: Mepivacaine hydrochloride

描述: Mepivacaine hydrochloride (Mepivacaine HCl) 是具有局部麻醉特性的酰胺衍生物。Mepivacaine hydrochloride 与神经元细胞膜上特定的电压门控钠离子通道结合，抑制钠离子内流和膜去极化。

激酶实验: Phosphatase Assay: Purified bovine brain calcineurin and calmodulin are purchased. Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μl (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCI, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per ml, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μl of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μl of assay buffer. Where indicated, reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 ml of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described.

体内活性: 在马匹进行的测试表明，mepivacaine在相邻滑膜结构间的扩散比从先前的解剖学、乳胶注射及对比关节造影研究所假设的要广泛。[1] 超声波在减少进行膝关节镜手术的患者所需的最小有效麻醉体积（MEAV50）方面表现出色。与神经刺激相比，使用1.5% mepivacaine时可降低37%。[2] 使用3% mepivacaine提供的麻醉持续时间比带有肾上腺素的lidocaine配方在犬齿和前磨牙中更短。[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3 mg/mL (10.6 mM)
Ethanol : 8 mg/mL (28.28 mM)
H2O : 52 mg/mL (183.9 mM)


关键字: regional | inhibit | Mepivacaine hydrochloride | Sodium Channel | Mepivacaine | Na channels | local | infiltration | Inhibitor | Mepivacaine Hydrochloride | Na+ channels | neuronal | cell | depolarization | anesthetic | amide-type

相关产品: Ropivacaine | ProTx-III | µ-Conotoxin SIIIA | Transcainide | Piromelatine | Ancistrotecine B | Clopamide | Nav1.8-IN-4 | SM-6586 | Diphenidol hydrochloride

相关库: Ion Channel Inhibitor Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library | Anti-Cancer Approved Drug Library | Sodium Channel Blocker Library | Preclinical Compound Library | Bioactive Compound Library

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