Lidocaine hydrochloride (Lignocaine hydrochloride)
(Synonyms: 盐酸利多卡因; Lignocaine hydrochloride) 目录号 : GC33831
Lidocaine hydrochloride (Lignocaine hydrochloride)是一种氨基酰胺类局部麻醉剂,可抑制voltage-insensitive ‘flicker’ K+ channel,IC50值为220μM。
Cas No.:73-78-9
Sample solution is provided at 25 µL, 10mM.
Lidocaine hydrochloride (Lignocaine hydrochloride) is an amino-amide-type local anaesthetic that inhibits voltage-insensitive ‘flicker’ K+ channel with an IC50 value of 220μM[1]. Lidocaine hydrochloride can cross the blood-brain barrier through passive diffusion across membranes and cause the blockade of voltage-gated sodium channels (VGSCs), leading to a reversible block of action potential propagation [2]. Lidocaine hydrochloride has been widely used in disease models for pain suppression and anti-inflammatory and anti-injury[3].
In vitro, Lidocaine hydrochloride treatment for 24h inhibited the viability of CCD-1064sk cells with an IC50 value of 613.77µM[4]. Treatment of SH-SY5Y cells with 10mM Lidocaine hydrochloride for 24h resulted in morphological changes, induced apoptosis, and significantly increased the amount of LDH released into the culture medium[5]. Treatment with 5μM Lidocaine hydrochloride for 24h attenuated cytokine-induced endothelial and vascular smooth muscle cell injury and increased cell survival[6].
In vivo, Lidocaine hydrochloride treatment (30mg/kg; twice a week) via intraperitoneal injection for 30 days reduced the tumor growth of HepG2 cell xenografts in nude mice without affecting body weight[7]. Subcutaneous injection of Lidocaine hydrochloride (30mg/kg) at 12-hour intervals for 3 days rescued the contractile function of the ischemic myocardial region in a mouse model of persistent myocardial ischemia without affecting cardiomyocyte death[8].
References:
[1] Hermanns H, Hollmann M W, Stevens M F, et al. Molecular mechanisms of action of systemic lidocaine in acute and chronic pain: a narrative review[J]. British journal of anaesthesia, 2019, 123(3): 335-349.
[2] Moreira-Junior L, Leal-Cardoso J H, Cassola A C, et al. Eugenol and lidocaine inhibit voltage-gated Na+ channels from dorsal root ganglion neurons with different mechanisms[J]. Frontiers in Pharmacology, 2024, 15: 1354737.
[3] Karnina R, Arif S K, Hatta M, et al. Molecular mechanisms of lidocaine[J]. Annals of Medicine and Surgery, 2021, 69: 102733.
[4] Choi W, Ryu H, Fuwad A, et al. Quantitative analysis of the membrane affinity of local anesthetics using a model cell membrane[J]. Membranes, 2021, 11(8): 579.
[5] Friederich P, Schmitz T P. Lidocaine-induced cell death in a human model of neuronal apoptosis[J]. European journal of anaesthesiology, 2002, 19(8): 564-570.
[6] de Klaver M J M, Buckingham M G, Rich G F. Lidocaine attenuates cytokine-induced cell injury in endothelial and vascular smooth muscle cells[J]. Anesthesia & Analgesia, 2003, 97(2): 465-470.
[7] Xing W, Chen D T, Pan J H, et al. Lidocaine induces apoptosis and suppresses tumor growth in human hepatocellular carcinoma cells in vitro and in a xenograft model in vivo[J]. Anesthesiology, 2017, 126(5): 868-881.
[8] Müller-Edenborn B, Kania G, Osto E, et al. Lidocaine enhances contractile function of ischemic myocardial regions in mouse model of sustained myocardial ischemia[J]. PloS one, 2016, 11(5): e0154699.
Lidocaine hydrochloride (Lignocaine hydrochloride)是一种氨基酰胺类局部麻醉剂,可抑制voltage-insensitive ‘flicker’ K+ channel,IC50值为220μM[1]。Lidocaine hydrochloride通过被动扩散跨膜透过血脑屏障,阻断电压门控钠通道(VGSCs),导致动作电位传播的可逆性阻滞[2]。Lidocaine hydrochloride已广泛应用于疾病模型的镇痛、抗炎和抗损伤研究[3]。
在体外,Lidocaine hydrochloride处理24小时可抑制CCD-1064sk细胞活力,IC50值为613.77µM[4]。10mM的Lidocaine hydrochloride处理SH-SY5Y细胞24小时会引起形态学改变、诱导细胞凋亡,并显著增加培养基中LDH释放量[5]。5μM的Lidocaine hydrochloride处理24小时能减轻细胞因子诱导的内皮细胞和血管平滑肌细胞损伤,提高细胞存活率[6]。
在体内,裸鼠腹腔注射Lidocaine hydrochloride(30mg/kg;每周两次;持续30天)可抑制HepG2细胞异种移植瘤的生长且不影响体重[7]。持续性心肌缺血小鼠模型每隔12小时皮下注射30mg/kg剂量的Lidocaine hydrochloride(持续3天)能恢复缺血心肌区域的收缩功能,且不影响心肌细胞死亡[8]。
Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were cultured in Dulbecco's modified Eagle's medium (DMEM) containing 4.5g/L D-glucose and glutaMAX supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin. Cells were incubated under standard culture conditions (CO2 5%, O2 95%, 37°C), and experiments were performed at 70% to 100% confluency. MDA-MB-231 cells were cultured in six-well plates and incubated for 24 hours with Lidocaine hydrochloride (100μM). A scratch was created in each well using a small pipettor tip, and the migration of cells was stimulated with 0.1μM CXCL12, after which the scratch wound area was quantified. |
Reaction Conditions | 100μM; 24h |
Applications | Lidocaine hydrochloride treatment significantly inhibited CXCL12-induced in vitro migration of MDA-MB-231 cells. |
Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | HepG2 cells (2×106) were subcutaneously injected into the right axilla of BALB/c nude mice. The mice were randomly divided into a control group, Lidocaine hydrochloride group, and cisplatin group (n=8 in each group). When the palpable tumor volume reached approximately 50mm3, mice were intraperitoneally injected with PBS solution (as a control), Lidocaine hydrochloride (30mg/kg; twice a week), and cisplatin (3mg/kg; once a week), and tumor growth was observed for 30 days. Tumor width and length were measured every 3 days. Tumor volume was calculated as (length × width2)/2. The body weight of mice was also recorded. |
Dosage form | 3mg/kg; twice a week for 30 days; i.p. |
Applications | Lidocaine hydrochloride treatment inhibited the tumor growth of HepG2 cell xenografts in nude mice without affecting body weight. |
References: |
Cas No. | 73-78-9 | SDF | |
别名 | 盐酸利多卡因; Lignocaine hydrochloride | ||
Canonical SMILES | O=C(NC1=C(C)C=CC=C1C)CN(CC)CC.[H]Cl | ||
分子式 | C14H23ClN2O | 分子量 | 270.8 |
溶解度 | Water : ≥ 36 mg/mL (132.94 mM) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 3.6928 mL | 18.4638 mL | 36.9276 mL |
5 mM | 738.6 μL | 3.6928 mL | 7.3855 mL |
10 mM | 369.3 μL | 1.8464 mL | 3.6928 mL |
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