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VDM 11 (in Tocrisolve 100)
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), in
water-soluble emulsion (for details see Cat. No. 1684). IC50 values
for inhibition of AMT are 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 as pure oil dissolved in ethanol (Cat. No.
1392).
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.
