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Modulation of anxiety through blockade of anandamide hydrolysis
The results indicate that anandamide participates in the modulation of emotional states and point to fatty acid amide hydrolase inhibition as an innovative approach to anti-anxiety therapy.
Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α
The results, which show that OEA induces satiety by activating PPAR-α, identify an unexpected role for this nuclear receptor in regulating behaviour, and raise possibilities for the treatment of eating disorders, are identified.
An endocannabinoid mechanism for stress-induced analgesia
The results indicate that the coordinated release of 2-AG and anandamide in the periaqueductal grey matter might mediate opioid-independent stress-induced analgesia, and identify monoacylglycerol lipase as a previously unrecognized therapeutic target.
Characterization of the Fatty Acid Amide Hydrolase Inhibitor Cyclohexyl Carbamic Acid 3′-Carbamoyl-biphenyl-3-yl Ester (URB597): Effects on Anandamide and Oleoylethanolamide Deactivation
- D. Fegley, S. Gaetani, D. Piomelli
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 April 2005
The results suggest that an enzyme distinct from FAAH catalyzes OEA hydrolysis in the duodenum, where this lipid substance acts as a local satiety factor.
Correction for Gobbi et al., Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis
- G. Gobbi, F. Bambico, D. Piomelli
- BiologyProceedings of the National Academy of Sciences…
- 18 December 2005
It is shown that URB597, a selective inhibitor of the enzyme fatty-acid amide hydrolase, which catalyzes the intracellular hydrolysis of the endocannabinoid anandamide, exerts potent antidepressant-like effects in the mouse tail-suspension test and the rat forced-swim test.
Antidepressant-like Activity of the Fatty Acid Amide Hydrolase Inhibitor URB597 in a Rat Model of Chronic Mild Stress
Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597).
KDS-4103 acts by enhancing the tonic actions of anandamide on a subset of CB(1) receptors, which may normally be engaged in controlling emotions and pain, to offer a novel approach with a favorable therapeutic window for the treatment of anxiety, depression and pain.
Selective inhibition of 2-AG hydrolysis enhances endocannabinoid signaling in hippocampus
Two previously unknown inhibitors of monoacylglycerol lipase, a presynaptic enzyme that hydrolyzes 2-AG, increase 2- AG levels and enhance retrograde signaling from pyramidal neurons to GABAergic terminals in the hippocampus are shown.
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.
Fatty acid amide hydrolase (FAAH) is a promising target for modulating endocannabinoid and fatty acid ethanolamide signaling, which may have important therapeutic potential. We recently described a…
Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism
The results suggest that anandamide-mediated signaling at peripheral CB1 receptors controls the access of pain-related inputs to the CNS, and brain-impenetrant FAAH inhibitors, which strengthen this gating mechanism, might offer a new approach to pain therapy.