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Literature summary 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

Activating Compound

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 (5Z,8Z,11Z,14Z)-eicosantetraenoic acid 3-thienyl methyl ester i.e. CAY-10402, 14% inhibition at 0.1 mM Rattus norvegicus
3.1.1.23 1-(20-cyano-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol i.e. O-223 Rattus norvegicus
3.1.1.23 1-(20-hydroxy-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol i.e. O-224 Rattus norvegicus
3.1.1.23 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
3.1.1.23 1-nor-arachidonoyl-3-(2'3-dihydroxypropyl) urea i.e. O-1502, 39% inhibition at 0.1 mM Rattus norvegicus
3.1.1.23 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
3.1.1.23 alpha-methyl-1-arachidonoylglycerol IC50 value is 0.011 mM Rattus norvegicus
3.1.1.23 arachidonic acid IC50 value is 0.078 mM Rattus norvegicus
3.1.1.23 arachidonoyl glycine 42% inhibition at 0.1 mM Rattus norvegicus
3.1.1.23 arachidonoyl serinol IC50 value is 0.073 mM Rattus norvegicus
3.1.1.23 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
3.1.1.23 noladin ether IC50 value is 0.036 mM Rattus norvegicus
3.5.1.4 (5Z,8Z,11Z,14Z)-eicosantetraenoic acid 3-thienyl methyl ester i.e. CAY-10402, IC50: 0.010 mM, 37% inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 1-arachidonoylglycerol 42% inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 1-nor-arachidonoyl-3-(2'3-dihydroxypropyl) urea i.e. O-1502, complete inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 2-arachidonoylglycerol 37% inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 3'-carbamoyl-biphenyl-3-yl-cyclohexylcarbamate i.e. URB597, specific, complete inhibition at 0.001 mM Rattus norvegicus
3.5.1.4 alpha-methyl-1-arachidonoylglycerol IC50: 0.033 mM, complete inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 arachidonic acid IC50: 0.058 mM, complete inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 arachidonoyl glycine IC50: 0.0049 mM, complete inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 arachidonoyl serinol IC50: 0.078 mM, complete inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 noladin ether IC50: 0.003 mM, complete inhibition at 0.1 mM Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.23 0.0022
-
 2-oleoylglycerol pH 7.2, 37°C, cytosolic fraction Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.1.1.23 cytosol
-
 Rattus norvegicus 5829
-
3.5.1.4 membrane
-
 Rattus norvegicus 16020
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.1.23 2-oleoylglycerol + H2O Rattus norvegicus
-
 oleic acid + glycerol
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.23 Rattus norvegicus
-
 adult Sprague-Dawley rats
-
3.5.1.4 Rattus norvegicus
-
 adult Sprague-Dawley rats
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.5.1.4 partially by membrane fraction preparation Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.23 cerebellum
-
 Rattus norvegicus
-
3.5.1.4 cerebellum
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.1.1.23 2.04
-
 cytosolic fraction Rattus norvegicus
3.5.1.4 0.00074
-
 membrane fraction Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-oleoylglycerol + H2O
-
 Rattus norvegicus oleic acid + glycerol
-
 ?
3.5.1.4 anandamide + H2O i.e. arachidonoylethanolamide Rattus norvegicus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.23 MAGL
-
 Rattus norvegicus
3.1.1.23 monoacylglycerol lipase
-
 Rattus norvegicus
3.5.1.4 FAAH
-
 Rattus norvegicus
3.5.1.4 fatty acid amide hydrolase
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.23 37
-
 assay at Rattus norvegicus
3.5.1.4 37
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.23 7.2
-
 assay at Rattus norvegicus
3.5.1.4 7.2
-
 assay at Rattus norvegicus

Ki Value [mM]

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

pI Value

EC Number Organism Comment pI Value Maximum pI Value
3.1.1.23 Rattus norvegicus
-
-
 additional information

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 0.011
-
 IC50 value is 0.011 mM Rattus norvegicus alpha-methyl-1-arachidonoylglycerol
3.1.1.23 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
3.1.1.23 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
3.1.1.23 0.036
-
 IC50 value is 0.036 mM Rattus norvegicus noladin ether
3.1.1.23 0.073
-
 IC50 value is 0.073 mM Rattus norvegicus arachidonoyl serinol
3.1.1.23 0.078
-
 IC50 value is 0.078 mM Rattus norvegicus arachidonic acid
3.5.1.4 0.003
-
 IC50: 0.003 mM, complete inhibition at 0.1 mM Rattus norvegicus noladin ether
3.5.1.4 0.0049
-
 IC50: 0.0049 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonoyl glycine
3.5.1.4 0.01
-
 i.e. CAY-10402, IC50: 0.010 mM, 37% inhibition at 0.1 mM Rattus norvegicus (5Z,8Z,11Z,14Z)-eicosantetraenoic acid 3-thienyl methyl ester
3.5.1.4 0.033
-
 IC50: 0.033 mM, complete inhibition at 0.1 mM Rattus norvegicus alpha-methyl-1-arachidonoylglycerol
3.5.1.4 0.058
-
 IC50: 0.058 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonic acid
3.5.1.4 0.078
-
 IC50: 0.078 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonoyl serinol