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137-58-6 分子结构
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2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide

ChemBase编号:166
分子式:C14H22N2O
平均质量:234.33728
单一同位素质量:234.17321333
SMILES和InChIs

SMILES:
O=C(Nc1c(cccc1C)C)CN(CC)CC
Canonical SMILES:
CCN(CC(=O)Nc1c(C)cccc1C)CC
InChI:
InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)
InChIKey:
NNJVILVZKWQKPM-UHFFFAOYSA-N

引用这个纪录

CBID:166 http://www.chembase.cn/molecule-166.html

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名称和登记号

名称和登记号

名称 登记号
IUPAC标准名
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
IUPAC传统名
lignocaine
2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
商标名
Dalcaine
Lidoject-1
Lidoject-2
Octocaine
Xylocaine
Xylocaine-MPF
Xylocaine-MPF with Glucose
Octocaine-50
Octocaine-100
Xylocaine Test Dose
Xylocaine 5% Spinal
After Burn Double Strength Gel
After Burn Double Strength Spray
After Burn Gel
After Burn Spray
Alphacaine
Anestacon
Anestacon Jelly
Cappicaine
DermaFlex
Duncaine
Emla
Esracaine
Gravocain
Isicaina
Lanabiotic
Leostesin
Lidoderm
Lignocaine
Maricaine
Norwood Sunburn Spray
Rocephin Kit
Xylocaine Dental Ointment
Xylocaine Endotracheal
Xylocaine Viscous
Xylocard
Zilactin-L
Solarcaine
Solarcaine aloe extra burn relief cream
Solcain
Zingo
别名
2-Diethylamino-N-(2,6-dimethylphenyl)acetamide
Lidocaine
Dilocaine
L-Caine
Lidocaine
N1-(2,6-Dimethylphenyl)-N2,N2-diethylglycinamide
Alphacaine
Xylocaine
lignocaine
Lidocaine(Alphacaine)
2-(Diethylamino)-2',6'-Acetoxylidide
''N''-(2,6-dimethylphenyl)-''N''2,''N''2-diethylglycinamide
Broncaine
Xilina
Xycaine
Xyline
CAS号
137-58-6
EC号
205-302-8
MDL号
MFCD00026733
PubChem SID
46505060
160963629
24896272
24896480
PubChem CID
367
3676
CHEBI ID
6456
ATC码
D04AB01
C05AD01
C01BB01
S02DA01
N01BB02
CHEMBL
79
Chemspider ID
3548
DrugBank ID
DB00281
IUPHAR配体索引
2623
KEGG ID
D00358
美国药典/FDA物质标识码
98PI200987
维基百科标题
Lidocaine

理论计算性质

理论计算性质

JChem ALOGPS 2.1
Acid pKa 13.775423  质子受体
质子供体 LogD (pH = 5.5) 0.6099084 
LogD (pH = 7.4) 2.329713  Log P 2.8429134 
摩尔折射率 73.9296 cm3 极化性 27.641424 Å3
极化表面积 32.34 Å2 可自由旋转的化学键
里宾斯基五规则 true 
Log P 1.81  LOG S -2.6 
溶解度 5.93e-01 g/l 

分子性质

分子性质

理化性质 安全信息 药理学性质 产品相关信息 生物活性(PubChem)
溶解度
4100 mg/L expand 查看数据来源
外观
powder expand 查看数据来源
熔点
66-69°C expand 查看数据来源
68°C (154.4°F) expand 查看数据来源
沸点
180°C expand 查看数据来源
疏水性(logP)
2.1 expand 查看数据来源
保存条件
-20°C expand 查看数据来源
Room Temperature (15-30°C) expand 查看数据来源
保存注意事项
IRRITANT expand 查看数据来源
RTECS编号
AN7525000 expand 查看数据来源
欧盟危险性物质标志
有害性(Harmful) 有害性(Harmful) (Xn) expand 查看数据来源
MSDS下载
下载链接 expand 查看数据来源
下载链接 expand 查看数据来源
下载链接 expand 查看数据来源
德国WGK号
3 expand 查看数据来源
危险公开号
22 expand 查看数据来源
R:22 expand 查看数据来源
安全公开号
22-26-36 expand 查看数据来源
S:36/37/39 expand 查看数据来源
TSCA收录
false expand 查看数据来源
GHS危险品标识
GHS07 expand 查看数据来源
GHS警示词
Warning expand 查看数据来源
GHS危险声明
H302 expand 查看数据来源
个人保护装置
dust mask type N95 (US), Eyeshields, Faceshields, Gloves expand 查看数据来源
作用靶点
Histamine receptors expand 查看数据来源
给药途径
IV, subcutaneous, topical expand 查看数据来源
生物利用度
35% (oral)
3% (topical)
expand 查看数据来源
排泄
renal expand 查看数据来源
半衰期
1.5–2 hours expand 查看数据来源
代谢
Hepatic, 90% CYP1A2-mediated expand 查看数据来源
法定药品分级
Rx Only (U.S.) (excluding 1%) (US) expand 查看数据来源
S4 (Australia) expand 查看数据来源
妊娠期药物分类
A (Australia) expand 查看数据来源
B (US) expand 查看数据来源
相关基因信息
human ... CYP1A2(1544)rat ... Scnn1a(25122) expand 查看数据来源
生物活性机理
Potassium channel (K ATP and K Vol ) blocker expand 查看数据来源
级别
analytical standard expand 查看数据来源
成盐信息
Free Base expand 查看数据来源
质检报告
下载链接 expand 查看数据来源
包装
vial of 200 mg expand 查看数据来源
应用领域
Antiarrhythmic agent expand 查看数据来源
Local anaesthetic expand 查看数据来源
Pharmacopeia Traceability
traceable to BP 727 expand 查看数据来源
traceable to PhEur L0595000 expand 查看数据来源
traceable to USP 1366002 expand 查看数据来源
Empirical Formula (Hill Notation)
C14H22N2O expand 查看数据来源

详细说明

详细说明

MP Biomedicals MP Biomedicals DrugBank DrugBank Selleck Chemicals Selleck Chemicals Wikipedia Wikipedia Sigma Aldrich Sigma Aldrich
MP Biomedicals -  02190111 external link
Crystalline
DrugBank -  DB00281 external link
Item Information
Drug Groups approved
Description A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]
Indication For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Pharmacology Lidocaine is an anesthetic agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Lidocaine appears to be similar to that of procaine, procainamide and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. In contrast to the latter 3 drugs, Lidocaine in therapeutic doses does not produce a significant decrease in arterial pressure or in cardiac contractile force. In larger doses, lidocaine may produce circulatory depression, but the magnitude of the change is less than that found with comparable doses of procainamide.
Toxicity The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Affected Organisms
Humans and other mammals
Biotransformation Primarily hepatic.
Absorption Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
Half Life 109 minutes
Protein Binding 60-80%
Elimination Lidocaine and its metabolites are excreted by the kidneys.
Distribution * 0.7 to 2.7 L/kg [healthy volunteers]
Clearance * 0.64 +/- 0.18 L/min
References
Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846. [Pubmed]
Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com
Selleck Chemicals -  S1357 external link
Research Area: Neurological Disease
Biological Activity:
Lidocaine (Alphacaine)is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. [1] Histamine is responsible for many features of allergic reactions. Lidocaine (Alphacaine)is a second-generation antihistamine agent closely structurally related to tricyclic antidepressants such as imipramine, and distantly related to the atypical antipsychotic quetiapine, used to treat allergies. [2]
Sigma Aldrich -  L1026 external link
包装
Supplied in amber screw-cap vials
Biochem/physiol Actions
Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
Sigma Aldrich -  L7757 external link
Frequently Asked Questions
Live Chat and Frequently Asked Questions are available for this Product.
Biochem/physiol Actions
Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
Sigma Aldrich -  19543 external link
Biochem/physiol Actions
Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.

参考文献

参考文献

供应商提供 Google Scholar IconGoogle Scholar PubMed iconPubMed Google Books IconGoogle Books
  • Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846. Pubmed
  • Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508. Pubmed
  • http://en.wikipedia.org/wiki/Lidocaine
  • Harms, A.F. et al., J. Med. Chem., 1961, 4, 575, (synth, pharmacol)
  • Garland, W.A. et al., Biomed. Mass Spectrom., 1974, 1, 124, (ms)
  • Jones, R.L., J. Pharm. Sci., 1974, 63, 1170, (ir)
  • Yoo, C.S. et al., Acta Cryst. B, 1975, 31, 1354, (cryst struct)
  • Singh, S.P. et al., Spectrosc. Lett., 1979, 12, 95, (pmr)
  • Noneman, J.W. et al., Drug Treat. Card. Arrhythmias, 1983, 193, (rev, pharmacol)
  • Groeningsson, K. et al., Anal. Profiles Drug Subst., 1985, 14, 207, (rev)
  • Powell, M.F., Anal. Profiles Drug Subst., 1986, 15, 761, (rev)
  • Negwer, M., Organic-Chemical Drugs and their Synonyms, 6th edn., Akademie-Verlag, 1987, 3325, (synonyms)
  • Martindale, The Extra Pharmacopoeia, 30th edn., Pharmaceutical Press, 1993, 1010
  • Comer, A.M. et al., Drugs, 2000, 59, 245-249, (rev)
  • Lewis, R.J., Sax's Dangerous Properties of Industrial Materials, 8th edn., Van Nostrand Reinhold, 1992, DHK400; DHK600
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专利

专利

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