盐酸利多卡因

盐酸利多卡因用途

水合盐酸利多卡因(盐酸利多卡因水合物)抑制涉及复杂电压和使用依赖性的钠通道。水合盐酸利多卡因通过上调miR-145表达和进一步失活MEK/ERK和NF-κB信号通路,减少胃癌细胞的生长、迁移和侵袭。盐酸利多卡因水合物是一种酰胺衍生物,具有研究室性心律失常的潜力[1][2]。

盐酸利多卡因名称

[ CAS 号 ]:
6108-05-0

[ 中文名 ]:
盐酸利多卡因

[ 英文名 ]:
Lidocaine HCl

[中文别名 ]:

[英文别名 ]:

Xyloneural
MFCD00150329
Lidocaine Hydrochloride Monohydrate
Lidocaine hydrochloride anhydrous
EINECS 200-803-8
Xylocard
Linocaine hydrochloride
Lidocaine HCl

盐酸利多卡因生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> MAPK/ERK信号通路 >> MEK

研究领域 >> 心血管疾病

信号通路 >> MAPK/ERK信号通路 >> ERK

信号通路 >> 干细胞及 Wnt 通路 >> ERK

[ 靶点 ]

ERK

NF-κB

MEK

[体外研究]

利多卡因(利多卡因)(10 nM；48小时)显著减少细胞增殖[2]。利多卡因(1-10 nM；24-72小时)抑制细胞活力,在10%浓度下达到最大抑制效果 nM和治疗时间48 小时[2]。利多卡因(10 nM；48小时)显著增加凋亡细胞率[2]。利多卡因(10 nM；48小时)显著下调细胞周期蛋白D1,上调p21表达[2]。细胞增殖试验[2]细胞系：人胃癌细胞系MKN45浓度：10 nM培养时间：48小时结果：细胞增殖明显减少。细胞活力测定[2]细胞系：人胃癌细胞系MKN45浓度：1、5和10 nM培养时间：24、48、72小时结果：抑制MKN45细胞活力。凋亡分析[2]细胞系：人胃癌细胞系MKN45浓度：10 nM孵育时间：48h结果：明显提高凋亡细胞率。Western Blot分析[2]细胞系：人胃癌细胞系MKN45浓度：10 nM孵育时间：48小时结果：细胞周期蛋白D1显著下调,p21表达显著上调。

[体内研究]

利多卡因可导致大鼠完全可逆的尾神经阻滞。与热伤害性阻滞相比,利多卡因产生的机械伤害性阻滞起效较慢,恢复更快[3]。

[参考文献]

[1]. Cummins TR, et al. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.

[2]. Sui H, et al. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233.

[3]. Li Z, et al. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6.

盐酸利多卡因物理化学性质

[ 沸点 ]:
350.8ºC at 760 mmHg

[ 熔点 ]:
68.5ºC

[ 分子式 ]:
C₁₄H₂₅ClN₂O₂

[ 分子量 ]:
288.814

[ 闪点 ]:
166ºC

[ 精确质量 ]:
288.160461

[ PSA ]:
41.57000

[ LogP ]:
3.39440

[ 外观性状 ]:
固体

[ 储存条件 ]:
室温，干燥

[ 水溶解性 ]:
H2O: soluble

盐酸利多卡因MSDS

详细MSDS(安全技术说明书)

盐酸利多卡因毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AN7700000

CHEMICAL NAME :: 2',6'-Acetoxylidide, 2-(diethylamino)-, hydrochloride, hydrate

CAS REGISTRY NUMBER :: 6108-05-0

LAST UPDATED :: 199706

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C14-H22-N2-O.Cl-H.H2-O

MOLECULAR WEIGHT :: 288.86

WISWESSER LINE NOTATION :: 2N2&1VMR B1 F1 &GH &QH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 292 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 179,580,1971

盐酸利多卡因安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
UN 2811 6

[ WGK德国 ]:
3

[ RTECS号 ]:
AN7700000

[ 海关编码 ]:
2924299090

盐酸利多卡因海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

盐酸利多卡因文献

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J. Vet. Pharmacol. Ther. 38(1) , 35-40, (2015)

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Intravenous lidocaine decreases tumor necrosis factor alpha expression both locally and systemically in pigs undergoing lung resection surgery.

Anesth. Analg. 119(4) , 815-28, (2014)

Lung resection surgery is associated with an inflammatory reaction. The use of 1-lung ventilation (OLV) seems to increase the likelihood of this reaction. Different prophylactic and therapeutic measur...

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