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Literature summary extracted from

  • Vandevoorde, S.; Saha, B.; Mahadevan, A.; Razdan, R.K.; Pertwee, R.G.; Martin, B.R.; Fowler, C.J.
    Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase (2005), Biochem. Biophys. Res. Commun., 337, 104-109.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 1-arachidin 11% inhibition of the membraneous enzyme at 0.1 mM, 19% inhibition of the cytosolic enzyme at 0.1 mM Rattus norvegicus
3.1.1.23 1-arachidonoylglycerol IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 1-myristin IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 1-palmitin 44% inhibition of the membraneous enzyme at 0.1 mM, 38% inhibition of the cytosolic enzyme at 0.1 mM Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (11Z)-icos-11-enoate i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79% Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (5Z)-icos-5-enoate i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65% Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible Rattus norvegicus
3.1.1.23 additional information inhibitory potency of different 1-arachidonic acid analogues, the chain length of the fatty acid is important for affinity and inhibition, while methylations of the fatty acids do not influence the inhibitory potency, overview Rattus norvegicus
3.5.1.4 1-arachidin 10% inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 1-arachidonoylglycerol IC50: 0.0062 mM Rattus norvegicus
3.5.1.4 1-myristin IC50: 0.018, complete inhibition is possible Rattus norvegicus
3.5.1.4 1-palmitin IC50: 0.0080, complete inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (11Z)-icos-11-enoate i.e. O-4066, IC50: 0.010, complete inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate i.e. O-3907, IC50: 0.0057, complete inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate i.e. O-1428, 28% inhibition at 0.1 mM Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (5Z)-icos-5-enoate i.e. 3908, IC50: 0.011, 84% inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate i.e. O-3973, IC50: 0.0024, 95% inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate i.e. O-3832, IC50: 0.0076, complete inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate i.e. O-4081, IC50: 0.0051, 90% inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate i.e. O-3872, IC50: 0.014, complete inhibition is possible Rattus norvegicus
3.5.1.4 2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate i.e. 3846, IC50: 0.023, complete inhibition is possible Rattus norvegicus

Localization

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

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.23 brain
-
 Rattus norvegicus
-
3.5.1.4 brain
-
 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 MAGL-cy
-
 Rattus norvegicus
3.1.1.23 MAGL-m
-
 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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 0.0051
-
 IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate
3.1.1.23 0.0083
-
 i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate
3.1.1.23 0.0095
-
 IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible Rattus norvegicus 1-arachidonoylglycerol
3.1.1.23 0.011
-
 IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate
3.1.1.23 0.016
-
 i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate
3.1.1.23 0.017
-
 i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
3.1.1.23 0.026
-
 i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79% Rattus norvegicus 2,3-dihydroxypropyl (11Z)-icos-11-enoate
3.1.1.23 0.032
-
 IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible Rattus norvegicus 1-myristin
3.1.1.23 0.056
-
 i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65% Rattus norvegicus 2,3-dihydroxypropyl (5Z)-icos-5-enoate
3.1.1.23 0.071
-
 i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate
3.1.1.23 0.073
-
 i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate
3.5.1.4 0.0024
-
 i.e. O-3973, IC50: 0.0024, 95% inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate
3.5.1.4 0.0051
-
 i.e. O-4081, IC50: 0.0051 mM, 90% inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate
3.5.1.4 0.0057
-
 i.e. O-3907, IC50: 0.0057 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate
3.5.1.4 0.0062
-
 IC50: 0.0062 mM Rattus norvegicus 1-arachidonoylglycerol
3.5.1.4 0.0076
-
 i.e. O-3832, IC50: 0.0076 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
3.5.1.4 0.008
-
 IC50: 0.0080 mM, complete inhibition is possible Rattus norvegicus 1-palmitin
3.5.1.4 0.01
-
 i.e. O-4066, IC50: 0.010 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (11Z)-icos-11-enoate
3.5.1.4 0.011
-
 i.e. O-3908, IC50: 0.011 mM, 84% inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z)-icos-5-enoate
3.5.1.4 0.014
-
 i.e. O-3872, IC50: 0.014, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate
3.5.1.4 0.018
-
 IC50: 0.018 mM, complete inhibition is possible Rattus norvegicus 1-myristin
3.5.1.4 0.023
-
 i.e. 3846, IC50: 0.023, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate