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Merck
CN

N5536

Nefazodone hydrochloride

≥98% (HPLC), solid, selective serotonin reuptake inhibitor

别名:

2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl- 2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one hydrochloride, BMY-13754, MJ-13754-1, Serzone

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关于此项目

经验公式（希尔记法）:
C25H32ClN5O2 · HCl
化学文摘社编号:
82752-99-6
分子量:
506.47
MDL编号:
MFCD00935760
UNSPSC代码:
12352200
PubChem化学物质编号:
24724551
NACRES:
NA.77

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产品名称

Nefazodone hydrochloride, ≥98% (HPLC), solid

质量水平

100

方案

≥98% (HPLC)

表单

solid

储存条件

desiccated

颜色

white

溶解性

DMSO: ≥10 mg/mL
H2O: insoluble

创始人

Bristol-Myers Squibb

SMILES字符串

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)N=C(CC)N1CCOC4=CC=CC=C4.Cl

InChI

1S/C25H32ClN5O2.ClH/c1-2-24-27-31(25(32)30(24)18-19-33-23-10-4-3-5-11-23)13-7-12-28-14-16-29(17-15-28)22-9-6-8-21(26)20-22;/h3-6,8-11,20H,2,7,12-19H2,1H3;1H

InChI key

DYCKFEBIOUQECE-UHFFFAOYSA-N

基因信息

human ... HTR2A(3356), HTR2C(3358), SLC6A2(6530), SLC6A4(6532)

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相关类别

生化/生理作用

Novel antidepressant; mixed 5-HT2A serotonin receptor antagonist/serotonin uptake inhibitor.

特点和优势

This compound was developed by Bristol-Myers Squibb. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000321806
0000321806
0000247033
0000247032
0000147261

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S C Collins et al.
Diabetologia, 51(9), 1689-1693 (2008-07-16)
Long-term exposure to NEFAs leads to inhibition of glucose-induced insulin secretion. We tested whether the release of somatostatin and glucagon, the two other major islet hormones, is also affected. Mouse pancreatic islets were cultured for 72 h at 4.5 or
Jonathan N Bauman et al.
Drug metabolism and disposition: the biological fate of chemicals, 36(6), 1016-1029 (2008-03-12)
In vitro metabolism/bioactivation of structurally related central nervous system agents nefazodone (hepatotoxin) and aripiprazole (nonhepatotoxin) were undertaken in human liver microsomes in an attempt to understand the differences in toxicological profile. NADPH-supplemented microsomal incubations of nefazodone and glutathione generated conjugates
James A Dykens et al.
Toxicological sciences : an official journal of the Society of Toxicology, 103(2), 335-345 (2008-03-18)
Mitochondrial toxicity is increasingly implicated in a host of drug-induced organ toxicities, including hepatotoxicity. Nefazodone was withdrawn from the U.S. market in 2004 due to hepatotoxicity. Accordingly, we evaluated nefazodone, another triazolopyridine trazodone, plus the azaspirodecanedione buspirone, for cytotoxicity and
Nader Perroud et al.
Pharmacogenomics, 12(3), 365-377 (2011-04-01)
This study investigated clinical and genetic predictors of increasing suicidal ideation during antidepressant treatment. A total of 131 depressed outpatients were allocated to four antidepressants (paroxetine, venlafaxine, clomipramine or nefazodone) in a sequential step procedure until remission. Suicidality was assessed
R Davis et al.
Drugs, 53(4), 608-636 (1997-04-01)
Nefazodone hydrochloride is a phenylpiperazine antidepressant with a mechanism of action that is distinct from those of other currently available drugs. It potently and selectively blocks postsynaptic serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A receptors and moderately inhibits serotonin and noradrenaline (norepinephrine) reuptake.
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