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经验公式(希尔记法):
C13H8FNO5
化学文摘社编号:
分子量:
277.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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
SMILES string
Oc1cc(cc(c1O)[N+]([O-])=O)C(=O)c2ccccc2F
InChI key
RQPAUNZYTYHKHA-UHFFFAOYSA-N
form
solid
storage condition
protect from light
color
yellow
solubility
H2O: slightly soluble <0.7 mg/mL, 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 1.0 mg/mL, ethanol: soluble
storage temp.
2-8°C
Quality Level
Gene Information
human ... COMT(1312)
Application
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.
Biochem/physiol Actions
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.
Features and Benefits
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.
Disclaimer
Store tightly sealed at 4 °C, protected from exposure to light.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
J W Miller et al.
Clinical neuropharmacology, 20(1), 55-66 (1997-02-01)
L-Dopa is the most effective drug known for the treatment of Parkinson's disease. However, the large doses required to treat this neurodegenerative disorder can significantly affect tissue concentrations of sulfur amino acid metabolites due to peripheral and central O-methylation. These
A Storch et al.
Molecular pharmacology, 57(3), 589-594 (2000-02-29)
Inhibition of catechol-O-methyltransferase (COMT; EC 2.1.1.6) is a new therapeutic strategy in the treatment of Parkinson's disease. However, nothing is known about the effects of COMT inhibition on levodopa (L-dopa)-induced toxicity in dopamine (DA) neurons. Therefore we evaluated the effects
M H Hassan et al.
Human reproduction (Oxford, England), 26(11), 3008-3018 (2011-09-08)
Uterine leiomyomas (fibroids) are the most common pelvic tumors in women. We assessed the potential therapeutic utility of Ro 41-0960, a synthetic catechol-O-methyl transferase inhibitor (COMTI), in the Eker rat. We randomized uterine fibroid-bearing Eker rats for treatment with Ro
Mamoun M Alhamadsheh et al.
Science translational medicine, 3(97), 97ra81-97ra81 (2011-08-26)
A valine-to-isoleucine mutation at position 122 of the serum protein transthyretin (TTR), found in 3 to 4% of African Americans, alters its stability, leading to amyloidogenesis and cardiomyopathy. In addition, 10 to 15% of individuals older than 65 years develop
Majorie B M van Duursen et al.
Toxicological sciences : an official journal of the Society of Toxicology, 81(2), 316-324 (2004-07-16)
Phytochemicals are natural dietary constituents of fruits and vegetables. Some of these phytochemicals are known to affect estrogen-metabolizing enzymes. In breast tissue, estradiol can be metabolized to the catechol estrogens 2- and 4-hydroxyestradiol (2-OHE(2) and 4-OHE(2)). Catechol estrogens are suspected
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