Abstract | BACKGROUND AND PURPOSE: EXPERIMENTAL APPROACH: The hydrolysis of anandamide in homogenates and intact cells was measured using the substrate labelled in the ethanolamine part of the molecule. KEY RESULTS: Twenty compounds were tested. Among the commonly occurring flavonoids, kaempferol was the most potent, inhibiting FAAH in a competitive manner with a K(i) value of 5 microM. Among flavonoids with a more restricted distribution in nature, the two most active toward FAAH were 7-hydroxyflavone (IC(50) value of 0.5-1 microM depending on the solvent used) and 3,7-dihydroxyflavone (IC(50) value 2.2 microM). All three compounds reduced the FAAH-dependent uptake of anandamide and its metabolism by intact RBL2H3 basophilic leukaemia cells. CONCLUSIONS AND IMPLICATIONS:
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Authors | L Thors, M Belghiti, C J Fowler |
Journal | British journal of pharmacology
(Br J Pharmacol)
Vol. 155
Issue 2
Pg. 244-52
(Sep 2008)
ISSN: 0007-1188 [Print] England |
PMID | 18552875
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Arachidonic Acids
- Endocannabinoids
- Enzyme Inhibitors
- Flavonoids
- Kaempferols
- Polyunsaturated Alkamides
- kaempferol
- Amidohydrolases
- fatty-acid amide hydrolase
- anandamide
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Topics |
- Amidohydrolases
(antagonists & inhibitors)
- Arachidonic Acids
(metabolism)
- Endocannabinoids
- Enzyme Inhibitors
(chemistry, pharmacology)
- Flavonoids
(chemistry, pharmacology)
- Hydrolysis
- Kaempferols
(chemistry, pharmacology)
- Polyunsaturated Alkamides
(metabolism)
- Structure-Activity Relationship
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