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Literature summary for 3.1.1.23 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

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

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

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

Purification (Commentary)

Purification (Comment) Organism
partially purified Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
MGL
-
Rattus norvegicus
monoacylglycerol lipase
-
Rattus norvegicus

Ki Value [mM]

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