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Literature summary for 1.14.15.4 extracted from

  • Nagamine, S.; Horisaka, E.; Fukuyama, Y.; Maetani, K.; Matsuzawa, R.; Iwakawa, S.; Asada, S.
    Stereoselective reductive metabolism of metyrapone and inhibitory activity of metyrapone metabolites, metyrapol enantiomers, on steroid 11beta-hydroxylase in the rat (1997), Biol. Pharm. Bull., 20, 188-192.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
metyrapol 11beta-hydroxylase inhibition, 40.8% by racemate, 38.1% by (+)-enantiomer and 33.8% by (-)-enantiomer, each 0.4 mM Rattus norvegicus
Metyrapone 11beta-hydroxylase, 39.7% inhibition by 0.4 mM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
male Wistar
-

Source Tissue

Source Tissue Comment Organism Textmining
adrenal gland
-
Rattus norvegicus
-
liver
-
Rattus norvegicus
-
plasma pharmacokinetics of metyrapone and metyrapol Rattus norvegicus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.00968
-
+/-0.00126, 40.8% inhibition by 0.4 mM metyrapol, adrenal tissue Rattus norvegicus
0.00986
-
+/-0.00044, 39.7% inhibition by 0.4 mM metyrapone, adrenal tissue Rattus norvegicus
0.01011
-
+/-0.00126, 38.1% inhibition by 0.4 mM (+)-metyrapol, adrenal tissue Rattus norvegicus
0.01081
-
+/-0.00269, 33.8% inhibition by 0.4 mM (-)-metyrapol, adrenal tissue Rattus norvegicus
0.01633
-
+/-0.00237, no inhibitor, adrenal tissue Rattus norvegicus

Storage Stability

Storage Stability Organism
blood samples, 4°C Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11-deoxycorticosterone + reduced adrenal ferredoxin + O2 adrenal Rattus norvegicus corticosterone + oxidized adrenal ferredoxin + H2O
-
?
metyrapone + ? plasma, product-stereoselective reductive metabolism Rattus norvegicus metyrapol + ? enantiomers r

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Rattus norvegicus