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Literature summary for 3.5.1.4 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 3.5.1.4

Inhibitors

Inhibitors Comment Organism Structure
(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
1-arachidonoylglycerol 42% inhibition at 0.1 mM Rattus norvegicus
1-nor-arachidonoyl-3-(2'3-dihydroxypropyl) urea i.e. O-1502, complete inhibition at 0.1 mM Rattus norvegicus
2-arachidonoylglycerol 37% inhibition at 0.1 mM Rattus norvegicus
3'-carbamoyl-biphenyl-3-yl-cyclohexylcarbamate i.e. URB597, specific, complete inhibition at 0.001 mM Rattus norvegicus
alpha-methyl-1-arachidonoylglycerol IC50: 0.033 mM, complete inhibition at 0.1 mM Rattus norvegicus
arachidonic acid IC50: 0.058 mM, complete inhibition at 0.1 mM Rattus norvegicus
arachidonoyl glycine IC50: 0.0049 mM, complete inhibition at 0.1 mM Rattus norvegicus
arachidonoyl serinol IC50: 0.078 mM, complete inhibition at 0.1 mM Rattus norvegicus
noladin ether IC50: 0.003 mM, complete inhibition at 0.1 mM Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Rattus norvegicus 16020
-

Organism

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

Purification (Commentary)

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

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
0.00074
-
 membrane fraction Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anandamide + H2O i.e. arachidonoylethanolamide Rattus norvegicus ?
-
 ?

Synonyms

Synonyms Comment Organism
FAAH
-
 Rattus norvegicus
fatty acid amide hydrolase
-
 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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.003
-
 IC50: 0.003 mM, complete inhibition at 0.1 mM Rattus norvegicus noladin ether
0.0049
-
 IC50: 0.0049 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonoyl glycine
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
0.033
-
 IC50: 0.033 mM, complete inhibition at 0.1 mM Rattus norvegicus alpha-methyl-1-arachidonoylglycerol
0.058
-
 IC50: 0.058 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonic acid
0.078
-
 IC50: 0.078 mM, complete inhibition at 0.1 mM Rattus norvegicus arachidonoyl serinol