Application | Comment | Organism |
---|---|---|
medicine | there is significant therapeutic potential for FAAH inhibitors as analgesic, neuroprotective, anti-inflammatory and anti-anxiety drugs, and as agents for the treatment of metabolic and sleep disorders | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
recombinant expression of N-terminal maltose-binding protein fusion enzyme in CHO cells | Homo sapiens |
recombinant expression of transmembrane domain-deleted rat enzyme in Escherichia coli | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(6E,9E,12E,15E)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one | - |
Rattus norvegicus | |
3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate | irreversible inhibitor | Homo sapiens | |
3-phenylpropane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
4-(4-benzyloxyphenoxy)butanesulfonyl fluoride | - |
Rattus norvegicus | |
4-phenylbutane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
5-(4-benzyloxyphenyl)pentanesulfonyl fluoride | - |
Rattus norvegicus | |
5-(4-hydroxyphenyl)pentanesulfonyl fluoride | i.e. AM3506, irreversible inhibitor for both the rat and the human enzyme, that covalently modifies the enzyme | Homo sapiens | |
5-(4-hydroxyphenyl)pentanesulfonyl fluoride | i.e. AM3506, irreversible inhibitor for both the rat and the human enzyme | Rattus norvegicus | |
5-phenylpentane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
6-phenylhexane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
7-(2-benzyloxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-(2-hydroxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-(3-benzyloxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-(3-hydroxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-(4-benzyloxyphenyl)heptane-1-sulfonic acid methyl ester | - |
Rattus norvegicus | |
7-(4-benzyloxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-(4-hydroxyphenyl)heptanesulfonyl fluoride | - |
Rattus norvegicus | |
7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one | reversible inhibitor | Homo sapiens | |
7-phenylheptane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
8-phenyloctane-1-sulfonyl fluoride | - |
Rattus norvegicus | |
hexadecyl sulfonylfluoride | i.e. AM374, is a potent irreversible in vitro and in vivo inhibitor of fatty acid amide hydrolase | Homo sapiens | |
hexadecyl sulfonylfluoride | i.e. AM374, is a potent in vitro and in vivo inhibitor of fatty acid amide hydrolase | Rattus norvegicus | |
methyl arachidonoyl fluorophosphonate | - |
Homo sapiens | |
methyl arachidonoyl fluorophosphonate | - |
Rattus norvegicus | |
additional information | sulfonyl fluoride inhibitors of fatty acid amide hydrolase, structure-activity relationship, docking and molecular modeling, overview | Homo sapiens | |
additional information | sulfonyl fluoride inhibitors of fatty acid amide hydrolase, structure-activity relationship, docking and molecular modeling, overview | Rattus norvegicus | |
phenylmethane sulfonyl fluoride | irreversible inhibition | Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
64391 | - |
x * 64391, recombinant transmembrane domain-deleted enzyme mutant, mass spectrometry | Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
anandamide + H2O | Rattus norvegicus | - |
ethanolamine + arachidonic acid | - |
? | |
anandamide + H2O | Homo sapiens | - |
ethanolamine + arachidonic acid | - |
? | |
oleamide + H2O | Rattus norvegicus | - |
oleic acid + NH3 | - |
? | |
oleamide + H2O | Homo sapiens | - |
oleic acid + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O00519 | - |
- |
Rattus norvegicus | P97612 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
anandamide + H2O | - |
Rattus norvegicus | ethanolamine + arachidonic acid | - |
? | |
anandamide + H2O | - |
Homo sapiens | ethanolamine + arachidonic acid | - |
? | |
arachidonyl-7-amino-4-methylcoumarin amide + H2O | fluorogenic substrate | Rattus norvegicus | arachidonic acid + 7-amino-4-methylcoumarin | - |
? | |
arachidonyl-7-amino-4-methylcoumarin amide + H2O | fluorogenic substrate | Homo sapiens | arachidonic acid + 7-amino-4-methylcoumarin | - |
? | |
oleamide + H2O | - |
Rattus norvegicus | oleic acid + NH3 | - |
? | |
oleamide + H2O | - |
Homo sapiens | oleic acid + NH3 | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 64391, recombinant transmembrane domain-deleted enzyme mutant, mass spectrometry | Rattus norvegicus |
Synonyms | Comment | Organism |
---|---|---|
FAAH | - |
Rattus norvegicus |
FAAH | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Rattus norvegicus |
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Rattus norvegicus |
7.4 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000012 | - |
pH 7.4, 25°C | Rattus norvegicus | 4-(4-benzyloxyphenoxy)butanesulfonyl fluoride | |
0.0000012 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(2-hydroxyphenyl)heptanesulfonyl fluoride | |
0.0000015 | - |
pH 7.4, 25°C | Rattus norvegicus | 5-(4-benzyloxyphenyl)pentanesulfonyl fluoride | |
0.0000022 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(4-hydroxyphenyl)heptanesulfonyl fluoride | |
0.0000025 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(3-hydroxyphenyl)heptanesulfonyl fluoride | |
0.0000028 | - |
pH 7.4, 25°C | Rattus norvegicus | 5-(4-hydroxyphenyl)pentanesulfonyl fluoride | |
0.0000036 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(3-benzyloxyphenyl)heptanesulfonyl fluoride | |
0.0000037 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(4-benzyloxyphenyl)heptanesulfonyl fluoride | |
0.0000043 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(2-benzyloxyphenyl)heptanesulfonyl fluoride | |
0.0000051 | - |
pH 7.4, 25°C | Homo sapiens | 5-(4-hydroxyphenyl)pentanesulfonyl fluoride | |
0.000037 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-phenylheptane-1-sulfonyl fluoride | |
0.000038 | - |
pH 7.4, 25°C | Rattus norvegicus | 6-phenylhexane-1-sulfonyl fluoride | |
0.00005 | - |
pH 7.4, 25°C | Rattus norvegicus | 5-phenylpentane-1-sulfonyl fluoride | |
0.000088 | - |
pH 7.4, 25°C | Rattus norvegicus | 4-phenylbutane-1-sulfonyl fluoride | |
0.000176 | - |
pH 7.4, 25°C | Rattus norvegicus | 8-phenyloctane-1-sulfonyl fluoride | |
0.000205 | - |
pH 7.4, 25°C | Rattus norvegicus | 3-phenylpropane-1-sulfonyl fluoride | |
0.000269 | - |
pH 7.4, 25°C | Rattus norvegicus | 7-(4-benzyloxyphenyl)heptane-1-sulfonic acid methyl ester |
General Information | Comment | Organism |
---|---|---|
malfunction | enzyme inhibition and deficiency causes increased central and peripheral neuronal levels of anandamide and other FAAs producing physiological effects including analgesia, apoptosis in various cancer cells, 12-14 modulation of memory processes, neuroprotection, epilepsy, feeding, and prevention of neurotoxicity of the human amyloid-beta peptide in Alzheimer's disease. Also anti-depressant, anxiolytic, antiinflammatory, anti-hypertensive, gastrointestinal and sleep-inducing effects are observed | Homo sapiens |
additional information | the mammalian enzyme is in the amidase signature (AS) family bearing the unusual Ser-Ser-Lys catalytic triad | Rattus norvegicus |
additional information | the mammalian enzyme is in the amidase signature (AS) family bearing the unusual Ser-Ser-Lys catalytic triad | Homo sapiens |
physiological function | the enzyme degrades and inactivates members of the fatty acid amide family of endogenous signaling lipids, including anandamide and oleamide. Anandamide binds and activates the CB1 and CB2 cannabinoid receptors, the molecular targets of plant-derived (-)-DELTA9-terahydrocannabinol, while oleamide induces physiological sleep and modulates serotonergic systems and GABAergic transmission | Homo sapiens |
physiological function | the enzyme degrades and inactivates members of the fatty acid amide family of endogenous signaling lipids, including anandamide and oleamide. Anandamide binds and activates the CB1 and CB2 cannabinoid receptors, the molecular targets of plant-derived (?)-DELTA9-terahydrocannabinol, while oleamide induces physiological sleep and modulates serotonergic systems and GABAergic transmission | Rattus norvegicus |