VDM 11 (in Tocrisolve™ 100)
Discontinued Product
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 TocrisoveTM 100). IC50 values for inhibition of AMT are 4 - 11 mM. Displays negligible agonist activity at the hVR1 receptor and very weak action at CB1 and CB2 receptors. Ki values are > 5 - 10 mM at CB1 and CB2. Active in vivo.VDM 11, pure oil dissolved in ethanol and Tocrisolve Control also available.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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The uptake by cells of 2-arachidonoylglycerol, an endogenous agonist of cannabinoid receptors.
Bisogno et al.
Eur.J.Biochem., 2001;268:1982 -
The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism.
De Petrocellis et al.
J.Biol.Chem., 2001;276:12856 -
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity.
De Petrocellis et al.
FEBS Lett., 2000;483:52 -
Experimental Parkinsonism alters endocannabinoid degradation: implications for striatal glutamatergic transmission.
Gubellini et al.
J.Neurosci., 2002;22:6900
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