R108
Ro 41-0960
solid
别名:
2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone
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关于此项目
经验公式（希尔记法）:
C13H8FNO5
化学文摘社编号:
分子量:
277.20
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
表单
solid
质量水平
储存条件
protect from light
颜色
yellow
溶解性
H2O: slightly soluble <0.7 mg/mL
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 1.0 mg/mL
ethanol: soluble
储存温度
2-8°C
SMILES字符串
Oc1cc(cc(c1O)[N+]([O-])=O)C(=O)c2ccccc2F
InChI
1S/C13H8FNO5/c14-9-4-2-1-3-8(9)12(17)7-5-10(15(19)20)13(18)11(16)6-7/h1-6,16,18H
InChI key
RQPAUNZYTYHKHA-UHFFFAOYSA-N
基因信息
human ... COMT(1312)
相关类别
应用
Ro 41-0960 has been used as an inhibitor of catechol-O-methyl-transferase in synaptosome membrane preparations and 3T3-L1 adipocytes. It has also been used as a catechol-O-methyl-transferase inhibitor to treat corpus striatum samples to test its effect on dopamine metabolism.
生化/生理作用
Ro 41-0960 is a specific and synthetic inhibitor of the enzyme catechol-O-methyl-transferase (COMT). It binds to the catalytic site and triggers the inhibition of the methylation property of COMT. Ro 41-0960 is effective on uterine leiomyoma lesions and uterine fibroids.
特点和优势
This compound is featured on the Dopamine and Norepinephrine Metabolism page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
免责声明
Store tightly sealed at 4 °C, protected from exposure to light.
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
新产品
Tiffany L Graves et al.
Analytical biochemistry, 373(2), 296-306 (2007-11-22)
A high-throughput, competitive fluorescence polarization immunoassay has been developed for the detection of methyltransferase activity. The assay was designed to detect S-adenosylhomocysteine (AdoHcy), a product of all S-adenosylmethionine (AdoMet)-utilizing methyltransferase reactions. We employed commercially available anti-AdoHcy antibody and fluorescein-AdoHcy conjugate
M Törnwall et al.
Pharmacology & toxicology, 69(1), 64-70 (1991-07-01)
3-Nitropyrocatechols are very potent and selective inhibitors of catechol-O-methyltransferase (COMT). LD50 values of three of these compounds were assessed after intraperitoneal administration with a special emphasis on interactions with drugs increasing catecholaminergic neurotransmission. LD50 values of the inhibitors varied from
M Törnwall et al.
Archives internationales de pharmacodynamie et de therapie, 320, 5-20 (1992-11-01)
The effects of three new catechol O-methyltransferase (COMT) inhibitors (nitecapone, entacapone and Ro 41-0960) were assessed on brain neurochemistry and psychomotor tests in levodopa/carbidopa-treated rats and mice. In neurochemical studies in rats, neither nitecapone (3 mg/kg) nor Ro 41-0960 (3
Thijs Beuming et al.
Nature neuroscience, 11(7), 780-789 (2008-06-24)
Cocaine is a widely abused substance with psychostimulant effects that are attributed to inhibition of the dopamine transporter (DAT). We present molecular models for DAT binding of cocaine and cocaine analogs constructed from the high-resolution structure of the bacterial transporter
Mu-Fa Zou et al.
Journal of medicinal chemistry, 60(24), 10172-10187 (2017-12-12)
The development of medications to treat cocaine use disorders has thus far defied success, leaving this patient population without pharmacotherapeutic options. As the dopamine transporter (DAT) plays a prominent role in the reinforcing effects of cocaine that can lead to
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