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Literature summary for 1.4.3.4 extracted from

  • Palaska, E.; Aydin, F.; Ucar, G.; Erol, D.
    Synthesis and monoamine oxidase inhibitory activities of 1-thiocarbamoyl-3,5-diphenyl-4,5-dihydro-1H-pyrazole derivatives (2008), Arch. Pharm., 341, 209-215.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-thiocarbamoyl-3-(4-bromophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-bromophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-chlorophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-methylphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
1-thiocarbamoyl-3-(4-methylphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole monoamine oxidase A; monoamine oxidase B Rattus norvegicus
Clorgyline monoamine oxidase A Rattus norvegicus
additional information no inhibition: 1-thiocarbamoyl-3-phenyl-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole, thiocarbamoyl-3-phenyl-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole Rattus norvegicus
Pargyline monoamine oxidase B Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0215
-
p-tyramine monoamine oxidase A Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Rattus norvegicus 5739
-
mitochondrion
-
Homo sapiens 5739
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P27338
-
-
Rattus norvegicus P21396
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Rattus norvegicus
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet
-
Homo sapiens
-
liver
-
Rattus norvegicus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.043
-
substrate p-tyramine, monoamine oxidase A Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzylamine + H2O + O2 monoamine oxidase B Homo sapiens benzaldehyde + NH3 + H2O2
-
?
p-tyramine + H2O + O2 monoamine oxidase A Rattus norvegicus 4-hydroxyphenylethanal + NH3 + H2O2
-
?
p-tyramine + H2O + O2 monoamine oxidase B Rattus norvegicus 4-hydroxyphenylethanal + NH3 + H2O2
-
?

Synonyms

Synonyms Comment Organism
MAO
-
Homo sapiens
MAO-A
-
Rattus norvegicus
MAO-B
-
Rattus norvegicus
monoamine oxidase A
-
Rattus norvegicus
monoamine oxidase B
-
Rattus norvegicus
monoamine oxidase B
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00285
-
no preincubation, monoamine oxidase B Rattus norvegicus Pargyline
0.00405
-
no preincubation, monoamine oxidase B Rattus norvegicus Pargyline
0.00416
-
monoamine oxidase A Rattus norvegicus Clorgyline
0.00496
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.0067
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.0342
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.0382
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.0523
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.0638
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.065
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.069
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.2853
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-bromophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.402
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-bromophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.47
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.485
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.486
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.49
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-bromophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.499
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-bromophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.5
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.5
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.5
-
preincubation 60 min, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.501
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.51
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-bromophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.51
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-chlorophenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.513
-
no preincubation, monoamine oxidase A Rattus norvegicus 1-thiocarbamoyl-3-(4-methylphenyl)-5-(2-chloro-3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole
0.53
-
no preincubation, monoamine oxidase B Rattus norvegicus 1-thiocarbamoyl-3-(4-methoxyphenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazole