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Literature summary extracted from

  • Magrioti, V.; Naxakis, G.; Hadjipavlou-Litina, D.; Makriyannis, A.; Kokotos, G.
    A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity (2008), Bioorg. Med. Chem. Lett., 18, 5424-5427.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.1.1.23 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

EC Number Inhibitors Comment Organism Structure
3.1.1.23 (2R,9Z)-octadec-9-ene-1,2-diamine dihydrochloride inhibits by 42.2% Rattus norvegicus
3.1.1.23 (2S)-6-[4-(hexyloxy)phenyl]hexane-1,2-diamine exhibits weak inhibitory activity (25.9%) Rattus norvegicus
3.1.1.23 (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
3.1.1.23 (R)-2-aminohexadecanol inhibits by 30% Rattus norvegicus
3.1.1.23 (S)-2-aminohexadecanol inhibits by 31.5% Rattus norvegicus
3.1.1.23 1,2-diaminohexadecane inhibits by 30.3% Rattus norvegicus
3.1.1.23 additional information (2S)-6-phenylhexane-1,2-diamine and (2S,9Z)-2-aminooctadec-9-enamide show no inhibition Rattus norvegicus
3.1.1.23 N-(2-hydroxyethyl)-2-oxopentadecanamide exhibits weak inhibitory activity (27.5%) and no selectivity towards MGL Rattus norvegicus

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.23 partially purified Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.23 brain
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-arachidonoylglycerol + H2O
-
 Rattus norvegicus arachidonic acid + glycerol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.23 MGL
-
 Rattus norvegicus
3.1.1.23 monoacylglycerol lipase
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.23 0.0218
-
 (2S,9Z)-octadec-9-ene-1,2-diamine
-
 Rattus norvegicus
3.1.1.23 0.039
-
 (2R,9Z)-octadec-9-ene-1,2-diamine dihydrochloride
-
 Rattus norvegicus
3.1.1.23 0.0587
-
 1,2-diaminohexadecane
-
 Rattus norvegicus