Cat. No. 1392
Chemical Name: (5Z,8Z,11Z,14Z)-N-(4-Hydroxy-2-meth
Biological ActivityA 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).
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Gubellini et al (2002) Experimental Parkinsonism alters endocannabinoid degradation: implications for striatal glutamatergic transmission. J.Neurosci. 22 6900. PMID: 12177188.
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 (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.
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.
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Citations are publications that use Tocris products. Selected citations for VDM 11 include:
Buznikov et al (2010) A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Dev Neurosci 32 1. PMID: 19907129.
Hillard et al (2007) Inhibition of 2-arachidonoylglycerol catabolism modulates vasoconstriction of rat middle cerebral artery by the thromboxane mimetic, U-46619. Br J Pharmacol 152 691. PMID: 17891162.
Newman et al (2007) Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction. Eur J Neurosci 25 1619. PMID: 17408433.
Battista et al (2002) Anandamide uptake by synaptosomes from human, mouse and rat brain: inhibition by glutamine and glutamate. Cereb Cortex 1 1. PMID: 12617751.
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Keywords: VDM 11, supplier, Potent, selective, anandamide, transporters, inhibitors, inhibits, AMT, Cannabinoids, Monoamine, Neurotransmitter, VDM11, Tocris Bioscience, Cannabinoid Transporter Inhibitor products
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