Chemical Name:(5Z,8Z,11Z,14Z)-N-(4-Hydroxy-2-methylphenyl)-5,8,11,14-
eicosatetraenamide
Biological Activity:
A potent and selective inhibitor of the
anandamide membrane transporter (AMT) with IC50 values of 4-11 μM. Displays
negligible agonist activity at the hVR1 receptor and very weak action at CB1
and CB2 receptors. Ki values are > 5-10 μM at CB1
and CB2. Active in vivo. Also available in water-soluble emulsion
(Cat. No. 1686).
De Petrocelliset al
(2000) Overlap between the ligand recognition properties of the anandamide
transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake
with negligible capsaicin-like activity. FEBS Lett. 483 52. De
Petrocelliset al (2001) The activity of anandamide at vanilloid VR1
receptors requires facilitated transport across the cell membrane and is
limited by intracellular metabolism. J.Biol.Chem. 276 12856. Bisognoet al (2001) The uptake by cells of 2-arachidonoylglycerol, an
endogenous agonist of cannabinoid receptors. Eur.J.Biochem. 268
1982.Gubelliniet al (2002)
Experimental Parkinsonism alters endocannabinoid degradation: implications for
striatal glutamatergic transmission. J.Neurosci. 22 6900.
