HU-211, a nonpsychotropic cannabinoid, rescues cortical neurones from excitatory amino acid toxicity in culture
| Autor: | Sarina Striem, Nomi Eshhar, Anat Biegon |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Cell Survival
medicine.medical_treatment Kainate receptor AMPA receptor Pharmacology Biology Receptors N-Methyl-D-Aspartate Neuroprotection Rats Sprague-Dawley Radioligand Assay chemistry.chemical_compound medicine Animals Dronabinol Amino Acids Dexanabinol Cells Cultured Cerebral Cortex Neurons Membranes Cannabinoids General Neuroscience Glutamate receptor Immunohistochemistry Rats Metabotropic receptor nervous system chemistry Phosphopyruvate Hydratase NMDA receptor Cannabinoid Dizocilpine Maleate Neuroscience |
| Zdroj: | NeuroReport. 5:237-240 |
| ISSN: | 0959-4965 |
| Popis: | The present study examined potential neuroprotective effects of HU-211, a synthetic non-psychotropic cannabinoid with non-competitive NMDA antagonist properties on neurones exposed to various excitotoxins in culture. HU-211 was found to protect neurones from NMDA and quisqualate-induced toxicity but not that produced by AMPA or kainate. NMDA-mediated neurotoxicity was blocked by HU-211 in a dose dependent manner with an EC50 = 3.8 +/- 0.9 microM. Radioligand binding studies have shown that HU-211 inhibits the binding of [3H]MK-801 to rat forebrain membranes (KI = 11.0 microM +/- 1.323) in a competitive manner, but was unable to displace [3H]kainate and [3H]AMPA binding. These data suggest that the neuroprotective activity of HU-211 is directly associated with the NMDA receptor channel and possibly with the quisqualate receptor of the metabotropic class. Thus, HU-211 appears to act as an NMDA open channel blocker and shows promise as a novel neuroprotectant for clinical use. |
| Databáze: | OpenAIRE |
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