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Literature summary for 2.1.1.6 extracted from

  • Kiss, L.E.; Ferreira, H.S.; Torrao, L.; Bonifacio, M.J.; Palma, P.N.; Soares-da-Silva, P.; Learmonth, D.A.
    Discovery of a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase (2010), J. Med. Chem., 53, 3396-3411.
    View publication on PubMed
Search for more literature for 2.1.1.6

Inhibitors

Inhibitors Comment Organism Structure
3,4,5-trihydroxypyrogallol liver homogenate, 0.03 mM inhibitor: 0.8% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
3-fluoro-4-[1-[4-(trifluoromethyl)phenyl]-1H-pyrazol-5-yl]benzene-1,2-diol liver homogenate, 0.03 mM inhibitor: 32.3% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
3-nitro-5-(1-p-tolyl-1H-pyrazol-5-yl)benzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 0% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
3-nitro-5-(1-phenyl-1H-pyrazol-5-yl)benzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 0% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
3-nitro-5-(1H-pyrazol-5-yl)benzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 0% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
4-(1-phenyl-1H-pyrazol-5-yl)benzene-1,2,3-triol liver homogenate, 0.03 mM inhibitor: 26.8% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
4-(5-(3,4-dihydroxy-5-nitrophenyl)-1H-pyrazol-1-yl)benzonitrile liver homogenate, 0.003 mM inhibitor: 0.3% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
4-[1-(4-methylphenyl)-1H-pyrazol-5-yl]benzene-1,2-diol liver homogenate, 0.03 mM inhibitor: 41.2% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
4-[4-(4-chlorophenyl)-5-methyl-1H-pyrazol-3-yl]benzene-1,2,3-triol liver homogenate, 0.003 mM inhibitor: 15.6% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
5-(1-methyl-1H-pyrazol-5-yl)-3-nitrobenzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 1.1% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
5-[1-(3-chlorophenyl)-1H-pyrazol-5-yl]-2,3-dihydroxybenzoic acid liver homogenate, 0.03 mM inhibitor: 24.1% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
5-[1-(3-chlorophenyl)-1H-pyrazol-5-yl]-3-nitrobenzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 0% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
5-[1-(3-chlorophenyl)-4-phenyl-1H-pyrazol-5-yl]-3-nitrobenzene-1,2-diol liver homogenate, 0.003 mM inhibitor: 68.6% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus
[5-(3,4-dihydroxy-5-nitrophenyl)-4-phenyl-1H-pyrazol-1-yl](4-methylphenyl)methanone liver homogenate, 0.003 mM inhibitor: 2.8% metanephrine formed relative to the control in absence of inhibitor (5 min reaction time), pH 7.8, 37°C Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
adrenaline + S-adenosyl-L-methionine
-
 Rattus norvegicus methanephrine + S-adenosyl-L-homocysteine
-
 ?

Synonyms

Synonyms Comment Organism
catechol-O-methyltransferase
-
 Rattus norvegicus