The Nonpsychotropic Cannabinoid Cannabidiol Modulates and Directly Activates Alpha-1 and Alpha-1-Beta Glycine Receptor Function.

Autor: Ahrens, Jörg, Demir, Reyhan, Leuwer, Martin, de la Roche, Jeanne, Krampfl, Klaus, Foadi, Nilufar, Karst, Matthias, Haeseler, Gertrud
Předmět:
Zdroj: Pharmacology; 2009, Vol. 83 Issue 4, p217-222, 6p, 3 Diagrams, 1 Graph
Abstrakt: Loss of inhibitory synaptic transmission within the dorsal horn of the spinal cord plays a key role in the development of chronic pain following inflammation or nerve injury. Inhibitory postsynaptic transmission in the adult spinal cord involves mainly glycine. Cannabidiol is a nonpsychotropic plant constituent of Cannabis sativa. As we hypothesized that non-CB receptor mechanisms of cannabidiol might contribute to its anti-inflammatory and neuroprotective effects, we investigated the interaction of cannabidiol with strychnine-sensitive α1 and α1β glycine receptors by using the whole-cell patch clamp technique. Cannabidiol showed a positive allosteric modulating effect in a low micromolar concentration range (EC50 values: α1 = 12.3 ± 3.8 μmol/l and α1β = 18.1 ± 6.2 μmol/l). Direct activation of glycine receptors was observed at higher concentrations above 100 μmol/l (EC50 values: α1 = 132.4 ± 12.3 μmol/l and α1β = 144.3 ± 22.7 μmol/l). These in vitro results suggest that strychnine-sensitive glycine receptors may be a target for cannabidiol mediating some of its anti-inflammatory and neuroprotective properties. Copyright © 2009 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index