Biological Activity
NMDA antagonist (IC50 = 11 μM for inhibition of [3H]MK-801 binding to rat forebrain membranes). Protects against NMDA- and quisqualate-induced neurotoxicity (EC50 = 3.8 μM) and enhances dopamine D1 receptor activity. Inhibits NF-κB, reducing TNF-α, IL-6 and nitric oxide production, and acts as a free radical scavenger. Exhibits beneficial effects in experimental models of multiple sclerosis, bacterial meningitis, septic shock, epilepsy, and traumatic and ischemic brain injury. Brain penetrant.
Technical Data
M. Wt | 386.57 |
Formula | C25H38O3 |
Storage | Store at -20°C |
Purity | ≥97% (HPLC) |
CAS Number | 112924-45-5 |
PubChem ID | 107778 |
InChI Key | SSQJFGMEZBFMNV-PMACEKPBSA-N |
Smiles | CCCCCCC(C)(C)C1=CC(O)=C([C@]2([H])[C@](C(C)(C)O3)([H])CC=C(CO)C2)C3=C1 |
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.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 38.66 | 100 | |
ethanol | 38.66 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 386.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.59 mL | 12.93 mL | 25.87 mL |
5 mM | 0.52 mL | 2.59 mL | 5.17 mL |
10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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References
References are publications that support the products' biological activity.
Eshhar et al (1993) HU-211, a non-psychotropic cannabinoid, rescues cortical neurones from excitatory amino acid toxicity in culture. Neuroreport 5 237 PMID: 8298080
Striem et al (1997) Interaction of dexanabinol (HU-211), a novel NMDA receptor antagonist, with the dopaminergic system. Eur.J.Pharmacol. 338 205 PMID: 9424014
Gallily et al (1997) Protection against septic shock and suppression of tumor necrosis factor α and nitric oxide production by dexanabinol (HU-211), a nonpsychotropic cannabinoid. J.Pharmacol.Exp.Ther. 283 918 PMID: 9353414
Juttler et al (2004) The cannabinoid dexanabinol is an inhibitor of the nuclear factor kappa B (NF-κB). Neuropharmacology 47 580 PMID: 15380375
Keywords: HU 211, supplier, NF-κB, NF-kappaB, NF-kB, inhibitors, inhibits, decreases, TNF-α, TNF-alpha, IL-6, NO, production, NMDA, antagonists, receptors, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, HU211, Dexanabinol, NMDA, Receptors, Tocris Bioscience