VDM 11 (in Tocrisolve™ 100)
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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
References are publications that support the biological activity of the product.
Bisogno et al (2001) The uptake by cells of 2-arachidonoylglycerol, an endogenous agonist of cannabinoid receptors. Eur.J.Biochem. 268 1982 PMID: 11277920
De Petrocellis et 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 PMID: 11033355
De Petrocellis et 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 PMID: 11278420
Gubellini et al (2002) Experimental Parkinsonism alters endocannabinoid degradation: implications for striatal glutamatergic transmission. J.Neurosci. 22 6900 PMID: 12177188
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