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Activation of the endocannabinoid system as a therapeutic approach in a murine model of multiple sclerosis
The results indicate that treatment during established disease significantly improves the motor function of the diseased mice and suggest that agents able to activate the endocannabinoid system could constitute a new series of drugs for the treatment of MS.
Comparison of anandamide transport in FAAH wild-type and knockout neurons: evidence for contributions by both FAAH and the CB1 receptor to anandamide uptake.
The results indicate that the protein-dependent uptake of AEA is largely mediated by known constituents of the endocannabinoid system (FAAH and the CB1 receptor), although a partial contribution of an additional UCM707-sensitive protein is also suggested.
Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitors.
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
It is hoped that these compounds, particularly the most potent in this series (compound 5, UCM707, with IC(50) values for anandamide uptake and FAAH of 0.8 and 30 microM, respectively), will provide useful tools for the elucidation of the role of the an andamide transporter system in vivo.
Arylpiperazine derivatives acting at 5-HT(1A) receptors.
The development of arylpiperazine derivatives acting at 5-HT(1A)Rs with an emphasis on structure-affinity relationships of agonists and antagonists, ligand-receptor interactions and pharmacological applications is reviewed.
Inhibition of Fatty Acid Amidohydrolase, the Enzyme Responsible for the Metabolism of the Endocannabinoid Anandamide, by Analogues of Arachidonoyl-serotonin
It is concluded that the 5-hydroxy group of arachidonoyl-serotonin contributes to, but is not essential for, inhibitory potency at fatty acid amidohydrolase.
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
A series of arachidonic acid derivatives of general structure I which have been characterized as highly potent and selective inhibitors of anandamide transporter deserves special attention as being the most potent endocannabinoid transporter inhibitor described to date.
Characterization of an anandamide degradation system in prostate epithelial PC‐3 cells: synthesis of new transporter inhibitors as tools for this study
PC‐3 cells possess a complete inactivation system for an andamide formed by an uptake process and the enzyme FAAH, suggesting a possible physiological function of anandamide in the prostate, reinforcing the role of endocannabinoid system as a neuroendocrine modulator.