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Merck
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文件

T9772

Sigma-Aldrich

三唑仑

别名:

8-Chloro-6-[2-chlorophenyl]-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine

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About This Item

经验公式（希尔记法）:
C17H12Cl2N4
CAS号:
28911-01-5
分子量:
343.21
EC號碼:
249-307-3
MDL號碼:
MFCD00079623
分類程式碼代碼:
12352200
PubChem物質ID:
24900602
NACRES:
NA.77

藥物控制

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)

溶解度

0.1 M HCl: soluble 1 g in 600 mL solvent
chloroform: soluble 1 g in 25 mL solvent
ethanol: soluble 1 g in 1000 mL solvent
DMSO: soluble 5.4 mg/mL
dichloromethane: 50 mg/mL, clear, colorless to faintly yellow
methanol: soluble 8.8 mg/mL
H2O: insoluble
diethyl ether: insoluble

起源

Johnson & Johnson

SMILES 字串

ClC1=CC=CC=C1C2=NCC3=NN=C(C)N3C4=CC=C(Cl)C=C42

InChI

1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3

InChI 密鑰

JOFWLTCLBGQGBO-UHFFFAOYSA-N

基因資訊

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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應用

Triazolam has been used to define nonspecific binding in radioligand binding assays. Triazolam has also been used to study the effects of reducing mPer1 mRNA levels in mouse cerbellum.

生化／生理作用

Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.

特點和優勢

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

準備報告

Triazolam is soluble in dichloromethane at 50 mg/ml, with heat as needed, yielding a clear, colorless to faint yellow solution. Furthermore, 1g of triazolam is soluble in 25 mL chloroform, 1000 mL ethanol, and 600 mL 0.1 M HCl. It is also soluble in DMSO (5.4 mg/ml) and methanol (8.8 mg/ml). However, it is insoluble in water and in ether.

象形圖

Health hazard
GHS08

訊號詞

Warning

危險聲明

H361fd

危險分類

Repr. 2

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 2

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)

分析证书(COA)

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R L Voorman et al.
The Journal of pharmacology and experimental therapeutics, 287(1), 381-388 (1998-10-09)
Administration of delavirdine, an HIV-1 reverse transcriptase inhibitor, to rats or monkeys resulted in apparent loss of hepatic microsomal CYP3A and delavirdine desalkylation activity. Human CYP3A catalyzes the formation of desalkyl delavirdine and 6'-hydroxy delavirdine, an unstable metabolite, while CYP2D6
M Akiyama et al.
British journal of pharmacology, 128(7), 1616-1622 (1999-12-22)
1. The mPer1 and mPer2 genes are putative mouse clock genes that regulate circadian oscillator present in the suprachiasmatic nucleus (SCN) neuron. While they are also expressed in the granular cell layer in the cerebellum, their function is unknown. In
G E Pakes et al.
Drugs, 22(2), 81-110 (1981-08-01)
Triazolam is a triazolobenzodiazepine with hypnotic properties, advocated for use in acute or chronic insomnia, situational insomnia in hospitalised patients, and insomnia associated with other disease states. As triazolam has a relatively short half-life of about 2 to 3 hours
R R Griffiths et al.
Neuroscience and biobehavioral reviews, 9(1), 133-151 (1985-01-01)
The abuse liability of a drug is a positive, interactive function of the reinforcing and adverse effects of the drug. The relative abuse liability of the hypnotic benzodiazepine, triazolam, has been controversial. This paper reviews animal and human studies bearing
Susan K Sullivan et al.
The Journal of pharmacology and experimental therapeutics, 311(2), 537-546 (2004-07-17)
Clinically used benzodiazepine and nonbenzodiazepine sedative-hypnotic agents for the treatment of insomnia produce their therapeutic effects through allosteric enhancement of the effects of the inhibitory neurotransmitter GABA at the GABA(A) receptor. Indiplon is a novel pyrazolopyrimidine sedative-hypnotic agent, currently in
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