Application | Comment | Organism |
---|---|---|
drug development | selective inhibitors of MGL may be valuable novel agents for the treatment of inflammatory pain. (2S,9Z)-octadec-9-ene-1,2-diamine is a selective inhibitor of MGL activity with in vivo analgesic and anti-inflammatory properties | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R,9Z)-octadec-9-ene-1,2-diamine dihydrochloride | inhibits by 42.2% | Rattus norvegicus | |
(2S)-6-[4-(hexyloxy)phenyl]hexane-1,2-diamine | exhibits weak inhibitory activity (25.9%) | Rattus norvegicus | |
(2S,9Z)-octadec-9-ene-1,2-diamine | selectively inhibits MGL by 49.9%. The presence of a long monounsaturated chain corresponding to oleic acid is a key requirement for the selective inhibition of MGL | Rattus norvegicus | |
(R)-2-aminohexadecanol | inhibits by 30% | Rattus norvegicus | |
(S)-2-aminohexadecanol | inhibits by 31.5% | Rattus norvegicus | |
1,2-diaminohexadecane | inhibits by 30.3% | Rattus norvegicus | |
additional information | (2S)-6-phenylhexane-1,2-diamine and (2S,9Z)-2-aminooctadec-9-enamide show no inhibition | Rattus norvegicus | |
N-(2-hydroxyethyl)-2-oxopentadecanamide | exhibits weak inhibitory activity (27.5%) and no selectivity towards MGL | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
SpragueDawley rats | - |
Purification (Comment) | Organism |
---|---|
partially purified | Rattus norvegicus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
2-arachidonoylglycerol + H2O | - |
Rattus norvegicus | arachidonic acid + glycerol | - |
? |
Synonyms | Comment | Organism |
---|---|---|
MGL | - |
Rattus norvegicus |
monoacylglycerol lipase | - |
Rattus norvegicus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0218 | - |
(2S,9Z)-octadec-9-ene-1,2-diamine | - |
Rattus norvegicus | |
0.039 | - |
(2R,9Z)-octadec-9-ene-1,2-diamine dihydrochloride | - |
Rattus norvegicus | |
0.0587 | - |
1,2-diaminohexadecane | - |
Rattus norvegicus |