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盐酸利多卡因

盐酸利多卡因用途

可用作控制室性心动过速，治疗室性早搏、室性心动过速和心室颤动等心律失常症状。

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 ]:

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]。

[ 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

Development and in vitro evaluation of a buccal drug delivery system based on preactivated thiolated pectin.

Drug Dev. Ind. Pharm. 40(11) , 1530-7, (2014)

The aim of this study was to evaluate the potential of preactivated thiolated pectin (Pec-Cys-MNA) for buccal drug delivery. Therefore, a gel formulation containing this novel polymer and the model dr...

Evaluation of regional limb perfusion with chloramphenicol using the saphenous or cephalic vein in standing horses.

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

Regional limb perfusion (RLP) significantly decreases morbidity and mortality associated with distal limb injuries in horses. There is an urgent need for finding additional effective antimicrobial dru...

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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