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Merck

R108

Ro 41-0960

solid

Synonym(s):

2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone

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About This Item

Empirical Formula (Hill Notation):
C13H8FNO5
CAS Number:
Molecular Weight:
277.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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color

yellow

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

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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J A Lavigne et al.
Cancer research, 61(20), 7488-7494 (2001-10-19)
Many of the major identified risk factors for breast cancer are associated with exposure to endogenous estrogen. In addition to the effects of estrogen as a growth factor, experimental and epidemiological evidence suggest that catechol metabolites of estrogen also contribute
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
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
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
Mathias E Jensen et al.
Neurochemistry international, 138, 104772-104772 (2020-05-29)
A solid body of preclinical evidence shows that glucagon-like peptide-1 receptor (GLP-1R) agonists attenuate the effects of substance use disorder related behaviors. The mechanisms underlying these effects remain elusive. In the present study, we hypothesized that GLP-1R activation modulates dopaminetransporter

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