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Merck
CN

C8414

Sigma-Aldrich

Clobazam

GABA receptor ligand, powder

别名:

7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione

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关于此项目

经验公式（希尔记法）:
C16H13ClN2O2
CAS Number:
22316-47-8
分子量:
300.74
EC 号:
244-908-7
MDL编号:
MFCD00079069
UNSPSC代码:
12352200
PubChem化学物质编号:
24893060
NACRES:
NA.77

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Product Name

Clobazam,

表单

powder

质量水平

200

药品控制

USDEA Schedule IV; Home Office Schedule 4.1; psychotrope (France); kontrollierte Droge in Deutschland; regulated under CDSA - not available from Sigma-Aldrich Canada; psicótropo (Spain); Decreto Lei 15/93: Tabela IV (Portugal); Pszichotróp anyag / Psychotropic Substance (Hungary), 78/2022. (XII. 28.) BM rendelet

SMILES字符串

CN1C(=O)CC(=O)N(c2ccccc2)c3cc(Cl)ccc13

InChI

1S/C16H13ClN2O2/c1-18-13-8-7-11(17)9-14(13)19(16(21)10-15(18)20)12-5-3-2-4-6-12/h2-9H,10H2,1H3

InChI key

CXOXHMZGEKVPMT-UHFFFAOYSA-N

基因信息

human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)

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一般描述

Clobazam is a benzodiazepine, comprising of B ring nitrogen placed in positions 1 and 5 contrary to 1,4-benzodiazepines. It is a ligand for γ-aminobutyric acid type A (GABAA) receptor and is metabolized by cytochrome P450 in the liver.

应用

Clobazam has been used as a benzodiazepine to test its effect on the activation of the human immunodeficiency virus type 1 (HIV-1) long terminal repeat (LTR).

生化/生理作用

Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
Clobazam interacts at α and γ2 subunits junction of the GABAA receptor. It is less sedative and elicits anxiolytic and anticonvulsant effects. Clobazam is more selective on the α2 subunit of the GABAA receptor than the α1 subunit. It is an antiseizure drug and is associated with antiepileptic activity. Clobazam is useful in treating chronic epileptic encephalopathy disorder, Lennox‐Gastaut syndrome. It is employed in epilepsy and seizure prevention adjunctive therapy.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302,H336,H412

危险分类

Acute Tox. 4 Oral - Aquatic Chronic 3 - STOT SE 3

靶器官

Respiratory system

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

Eyeshields, Gloves, type N95 (US)

法规信息

监管及禁止进口产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000258801
0000262486
0000262486
0000258801
078F0201

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Matilda Bäckberg et al.
Clinical toxicology (Philadelphia, Pa.), 57(3), 203-212 (2018-10-24)
In recent years, many unclassified benzodiazepines (BZD) have appeared through online sale as new psychoactive substances (NPS). This study describes bioanalytical and clinical data related to intoxications involving NPS BZD ("designer BZD") in the Swedish STRIDA project. Case series of
Clobazam: a safe, efficacious, and newly rediscovered therapeutic for epilepsy
Gauthier AC and Mattson RH
CNS Neuroscience & Therapeutics, 21(7), 543-548 (2015)
Benzodiazepines Drive Alteration of Chromatin at the Integrated HIV-1 LTR
Elbezanti W, et al.
Viruses, 12(2), 191-191 (2020)
Stefan Wolking et al.
Neurology, 92(11), e1238-e1249 (2019-02-10)
The aim of this study was to expand the spectrum of epilepsy syndromes related to STX1B, encoding the presynaptic protein syntaxin-1B, and establish genotype-phenotype correlations by identifying further disease-related variants. We used next-generation sequencing in the framework of research projects
A comprehensive overview of the clinical pharmacokinetics of clobazam
Tolbert Dand Larsen F
Journal of Clinical Pharmacology, 59(1), 7-19 (2019)
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