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
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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
[Na channel myotonia].
H Nemoto et al.
Ryoikibetsu shokogun shirizu, (35)(35), 140-143 (2001-09-15)
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
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
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
John C L Erve
Current drug metabolism, 9(2), 175-188 (2008-02-22)
Metabolism of xenobiotics can sometimes generate cyclic metabolites. Such metabolites are usually the result of intramolecular reactions occurring within a primary or secondary metabolite and this chemistry may lead to unexpected structures. Intramolecular chemistry is often driven by nucleophilic groups
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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