T0202
Tocainide 盐酸盐
≥98% (HPLC), sodium channel blocker, solid
别名:
2-Amino-N-(2,6-dimethylphenyl)propanamide 盐酸盐
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关于此项目
经验公式（希尔记法）:
C11H16N2O · HCl
化学文摘社编号:
分子量:
228.72
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
Tocainide 盐酸盐, ≥98% (HPLC), solid
质量水平
方案
≥98% (HPLC)
表单
solid
储存条件
desiccated
under inert gas
颜色
white
溶解性
DMSO: >20 mg/mL
H2O: ≥5 mg/mL
创始人
AstraZeneca
储存温度
2-8°C
SMILES字符串
Cl[H].CC(N)C(=O)Nc1c(C)cccc1C
InChI
1S/C11H16N2O.ClH/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12;/h4-6,9H,12H2,1-3H3,(H,13,14);1H
InChI key
AMZACPWEJDQXGW-UHFFFAOYSA-N
基因信息
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相关类别
应用
Tocainide hydrochloride may be used in cell signaling studies.
生化/生理作用
Tocainide hydrochloride is a primary amine analog of lidocaine (lignocaine), used for the treatment of tinnitus. It blocks the sodium channels in the pain-producing foci in the nerve membranes and renders an analgesic effect in trigeminal neuralgia.
Tocainide hydrochloride is a sodium channel blocker; Class IB antiarrhythmic.
特点和优势
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Tocainide is voltage-dependent and use-dependent sodium channel blocker (class IB type antiarrhythmic); Ki = 115 μM in blockade of inactivated-state sodium channels; IC50 = 985μM in blockade of Na+ currents at a holding potential (HP) of -140 mV; IC50 = 254 μM in blockade of Na+ currents at HP -70 mV; IC50 = 523 μM in blockade of Na+ currents at tonic block (-100 mV); IC50 = 248 μM for use-dependent block at 10 Hz.
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
法规信息
新产品
此项目有
P Lindström et al.
Pain, 28(1), 45-50 (1987-01-01)
Tocainide is a derivative of lidocaine with anti-arrhythmic action and, unlike lidocaine, can be used for oral treatment. Tocainide was alternatively with carbamazepine given to 12 patients with trigeminal neuralgia in a double-blind cross-over study for 2 weeks. The analgesic
[Na channel myotonia].
H Nemoto et al.
Ryoikibetsu shokogun shirizu, (35)(35), 140-143 (2001-09-15)
V Challapalli et al.
The Cochrane database of systematic reviews, (4)(4), CD003345-CD003345 (2005-10-20)
Lidocaine, mexiletine, tocainide, and flecainide are local anesthetics which give an analgesic effect when administered orally or parenterally. Early reports described the use of intravenous lidocaine or procaine to relieve cancer and postoperative pain (Keats 1951; Gilbert 1951; De Clive-Lowe
Hassan Y Aboul-Enein et al.
Journal of biochemical and biophysical methods, 54(1-3), 407-413 (2003-01-25)
Enantiomeric resolution of thyroxine and tocainide was achieved on a (+)-(18-crown-6)-2,3,11,12-tetracarboxylic acid column. The mobile phases were methanol/water (4:1, v/v) and methanol/water containing 5 mM sulfuric acid (4:1, v/v) for tocainide and thyroxine respectively. The flow rate was 0.5 ml/min.
Annamaria De Luca et al.
Molecular pharmacology, 64(4), 932-945 (2003-09-23)
Newly synthesized tocainide analogs were tested for their state-dependent affinity and use-dependent behavior on sodium currents (INa) of adult skeletal muscle fibers by means of the Vaseline-gap voltage clamp method. The drugs had the pharmacophore amino group constrained in position
商品
Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.
电压门控钠通道存在于大多数可兴奋细胞膜中，在产生动作电位方面起着重要作用。
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