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Literature summary for 3.1.1.23 extracted from

  • Ghafouri, N.; Tiger, G.; Razdan, R.K.; Mahadevan, A.; Pertwee, R.G.; Martin, B.R.; Fowler, C.J.
    Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol (2004), Br. J. Pharmacol., 143, 774-784.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.23

Activating Compound

Activating Compound Comment Organism Structure
ethanol activates 1.5fold at 5% v/v Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
(5Z,8Z,11Z,14Z)-eicosantetraenoic acid 3-thienyl methyl ester i.e. CAY-10402, 14% inhibition at 0.1 mM Rattus norvegicus
1-(20-cyano-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol i.e. O-223 Rattus norvegicus
1-(20-hydroxy-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol i.e. O-224 Rattus norvegicus
1-arachidonoylglycerol inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.017 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length Rattus norvegicus
1-nor-arachidonoyl-3-(2'3-dihydroxypropyl) urea i.e. O-1502, 39% inhibition at 0.1 mM Rattus norvegicus
2-arachidonoylglycerol inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.013 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length Rattus norvegicus
alpha-methyl-1-arachidonoylglycerol IC50 value is 0.011 mM Rattus norvegicus
arachidonic acid IC50 value is 0.078 mM Rattus norvegicus
arachidonoyl glycine 42% inhibition at 0.1 mM Rattus norvegicus
arachidonoyl serinol IC50 value is 0.073 mM Rattus norvegicus
arachidonoyl trifluoromethylketone the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length Rattus norvegicus
noladin ether IC50 value is 0.036 mM Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0022
-
 2-oleoylglycerol pH 7.2, 37°C, cytosolic fraction Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Rattus norvegicus 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2-oleoylglycerol + H2O Rattus norvegicus
-
 oleic acid + glycerol
-
 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
 adult Sprague-Dawley rats
-

Source Tissue

Source Tissue Comment Organism Textmining
cerebellum
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.04
-
 cytosolic fraction Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-oleoylglycerol + H2O
-
 Rattus norvegicus oleic acid + glycerol
-
 ?

Synonyms

Synonyms Comment Organism
MAGL
-
 Rattus norvegicus
monoacylglycerol lipase
-
 Rattus norvegicus

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
7.2
-
 assay at Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information
-
 Rattus norvegicus

pI Value

Organism Comment pI Value Maximum pI Value
Rattus norvegicus
-
-
 additional information

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.011
-
 IC50 value is 0.011 mM Rattus norvegicus alpha-methyl-1-arachidonoylglycerol
0.013
-
 inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.013 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length Rattus norvegicus 2-arachidonoylglycerol
0.017
-
 inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.017 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length Rattus norvegicus 1-arachidonoylglycerol
0.036
-
 IC50 value is 0.036 mM Rattus norvegicus noladin ether
0.073
-
 IC50 value is 0.073 mM Rattus norvegicus arachidonoyl serinol
0.078
-
 IC50 value is 0.078 mM Rattus norvegicus arachidonic acid