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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
275-361-2
MDL number:
产品名称
Tocainide 盐酸盐, ≥98% (HPLC), solid
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
SMILES string
Cl[H].CC(N)C(=O)Nc1c(C)cccc1C
assay
≥98% (HPLC)
form
solid
storage condition
desiccated, under inert gas
color
white
solubility
DMSO: >20 mg/mL, H2O: ≥5 mg/mL
originator
AstraZeneca
storage temp.
2-8°C
Quality Level
Gene Information
相关类别
Application
Tocainide hydrochloride may be used in cell signaling studies.
Biochem/physiol Actions
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.
Features and Benefits
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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
法规信息
新产品
此项目有
L He et al.
The Cochrane database of systematic reviews, (3)(3), CD004029-CD004029 (2006-07-21)
Non-antiepileptic drugs have been used in trigeminal neuralgia management since the 1970s. The objective was to review systematically the efficacy of non-antiepileptic drugs for trigeminal neuralgia. We searched the Cochrane Neuromuscular Disease Group Register, MEDLINE, EMBASE, and LILACS (all to
Antonio Carrieri et al.
European journal of medicinal chemistry, 44(4), 1477-1485 (2008-11-26)
Enantiomeric forms of Tocainide, Mexiletine, and structurally related local anaesthetic compounds, were analyzed with respect to their potency in blocking Na(v)1.4 channel. Structure-activity relationships based on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular
Alessia Catalano et al.
European journal of medicinal chemistry, 43(11), 2535-2540 (2008-03-18)
1-Benzyl-N-(2,6-dimethylphenyl)piperidine-3-carboxamide and 4-benzyl-N-(2,6-dimethylphenyl)piperazine-2-carboxamide, two conformationally restricted analogues of tocainide, were designed and synthesized as voltage-gated skeletal muscle sodium channel blockers. They showed, with respect to tocainide, a marked increase in both potency and use-dependent block.
Annamaria De Luca et al.
Neuromuscular disorders : NMD, 22(1), 56-65 (2011-08-02)
Drug screening on sodium currents of native myofibers by means of voltage-clamp recordings is predictive of pre-clinical anti-myotonic activity in vivo and ex vivo. By this approach we identified the N-benzylated beta-proline derivative of tocainide (To10) as the most potent
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
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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