R108
Ro 41-0960
solid
Synonyme(s) :
2′-Fluoro-3,4-dihydroxy-5-nitrobenzophenone
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A propos de cet article
Formule empirique (notation de Hill) :
C13H8FNO5
Numéro CAS:
Poids moléculaire :
277.20
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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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)
Catégories apparentées
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.
Classe de stockage
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
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
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
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
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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