Procaine hydrochloride

Procaine hydrochloride (Novocaine HCl) 是DNA 脱甲基剂,是一种苯甲酸衍生物,具有局部麻醉和抗心律失常特性。

CAS号

51-05-8

分子式

C13H20N2O2·HCl

主要靶点

DNA/RNA Synthesis|AChR|NMDAR|Histone Demethylase|Sodium Channel|5-HT Receptor

仅限科研使用

Cat No : CM00032

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Synonyms

盐酸普鲁卡因|Novocaine HCl|Procaine HCl



产品信息

Procaine Hydrochloride is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

CAS号 51-05-8
分子式 C13H20N2O2·HCl
主要靶点 DNA/RNA Synthesis|AChR|NMDAR|Histone Demethylase|Sodium Channel|5-HT Receptor
主要通路 表观遗传|离子通道|神经科学|细胞周期|DNA损伤和修复|G蛋白偶联受体
分子量 272.77
纯度 100.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 盐酸普鲁卡因|Novocaine HCl|Procaine HCl

靶点活性

5-HT3:1.7 μM(Kd)|nAChR:45.5 μM|NMDA Receptor:0.296 mM|sodium channel:60 μM

体内活性

Procaine具有结合或拮抗烟碱型乙酰胆碱受体和5-羟色胺受体-离子通道复合体与N-甲基-D-天冬氨酸受体的功能。Procaine主要通过抑制钠离子进而影响外周神经的神经元细胞膜上电压门控钠离子通道的内流来发挥作用。当钠离子内流被中断时,动作电位被阻断,信号传导也因此受到抑制。有研究认为受体部位是位于钠通道的细胞质(内部)部分。

体外活性

在清醒的猫体内,Procaine(15 mg/kg)增加杏仁核腹侧海马体,腹内侧下丘脑,伏隔核和颞叶新皮质的细胞活性.Procaine是边缘系统细胞的兴奋剂.Procaine促进诱发的刺激活性从杏仁核到腹内侧下丘脑的传导.

溶解度

H2O:50 mg/mL (183.3 mM),Ethanol:<1 mg/mL,DMSO:51 mg/mL (187 mM)

参考文献

1.Bräu ME ME, et al. Anesth Analg, 1998, 87(4), 885-889.
2.Hahnenkamp K, et al. Br J Anaesth, 2006, 96(1), 77-87.
3.Wang H, et al. Eur J Pharmacol, 2010, 630(1-3), 29-33.
4.Fan P, et al. Neuropharmacology, 1994, 33(12), 1573-1579.
5.Zahradníková A, et al. Biophys J. 1993 Apr;64(4):1991-12003.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2