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Literature summary for 3.5.1.99 extracted from

  • Wyffels, L.; Muccioli, G.G.; De Bruyne, S.; Moerman, L.; Sambre, J.; Lambert, D.M.; De Vos, F.
    Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain (2009), J. Med. Chem., 52, 4613-4622.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(5Z,8Z,11Z,14Z)-N-(2-hydroxyethyl)icosa-5,8,11,14-tetraenamide i.e. (5Z,8Z,11Z,14Z)-N-(2-hydroxyethyl)icosa-5,8,11,14-tetraenamide or N-arachidonoylethanolamine, competitive Mus musculus
2-iodobenzylarachidonoylamide
-
Mus musculus
2-iodobenzyllinoleoylamide
-
Mus musculus
2-iodophenethylarachidonoylamide
-
Mus musculus
2-iodophenethyllinoleoylamide
-
Mus musculus
2-methoxyphenethylarachidonoylamide
-
Mus musculus
2-methoxyphenethyllinoleoylamide
-
Mus musculus
3-iodobenzylarachidonoylamide
-
Mus musculus
3-iodobenzyllinoleoylamide
-
Mus musculus
3-iodophenethylarachidonoylamide
-
Mus musculus
3-iodophenethyllinoleoylamide
-
Mus musculus
3-methoxyphenethylarachidonoylamide
-
Mus musculus
3-methoxyphenethyllinoleoylamide
-
Mus musculus
4-iodobenzylarachidonoylamide
-
Mus musculus
4-iodobenzyllinoleoylamide
-
Mus musculus
4-iodophenethylarachidonoylamide
-
Mus musculus
4-iodophenethyllinoleoylamide
-
Mus musculus
4-methoxyphenethylarachidonoylamide
-
Mus musculus
4-methoxyphenethyllinoleoylamide
-
Mus musculus
methyl arachidonyl fluorophosphonate MAFP, a potent irreversible FAAH inhibitor Mus musculus
additional information synthesis of 18 aryl analogues of anandamide. In vitro evaluation of inhibitory potency, binding to CB1 and CB2 cannabinoid receptors, and potential as metabolic trapping tracers of 4-methoxyphenethyllinoleoylamide and 4-methoxyphenethylarachidonoylamide, overview Mus musculus
N-(2-hydroxyethyl)linoleoylamide competitive versus anadamide Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
anandamide + H2O Mus musculus
-
arachidonic acid + ethanolamine
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
male C75BL/6J mice
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anandamide + H2O
-
Mus musculus arachidonic acid + ethanolamine
-
?
N-(2-hydroxyethyl)linoleoylamide + H2O
-
Mus musculus ?
-
?

Synonyms

Synonyms Comment Organism
FAAH
-
Mus musculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Mus musculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6
-
assay at Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
pIC50, i.e. -log IC50. values of anadamide analogue inhibitors, overview Mus musculus additional information

General Information

General Information Comment Organism
physiological function importance of FAAH in controlling endogenous anandamide levels in the brain and consequently the importance of FAAH as a regulatory enzyme for key physiological functions. FAAH is one of the main enzymes responsible for terminating the signaling of endocannabinoids in the brain, it has a role in neuropsychiatric disorders Mus musculus