R108
Ro 41-0960
solid
Sinónimos:
2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone
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Acerca de este artículo
Fórmula empírica (notación de Hill):
C13H8FNO5
Número CAS:
Peso molecular:
277.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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Permítanos ayudarlecolor
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)
Categorías relacionadas
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.
Clase de almacenamiento
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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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
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.
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
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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