Modulation of Glycine Receptor Function by the Synthetic Cannabinoid HU210Demir R.a · Leuwer M.c · de la Roche J.a · Krampfl K.b · Foadi N.a · Karst M.a · Dengler R.b · Haeseler G.a · Ahrens J.a
aClinic for Anaesthesia and Critical Care Medicine, and bDepartment of Neurology and Neurophysiology, Hannover Medical School, Hannover, Germany; cDivision of Clinical Sciences, University of Liverpool, Liverpool, UK
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Article / Publication Details
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. HU210 is a non-psychotropic, synthetic cannabinoid. As we hypothesized that non-CB receptor mechanisms of HU210 might contribute to its anti-inflammatory and anti-nociceptive effects we investigated the interaction of HU210 with strychnine-sensitive α1 glycine receptors by using the whole-cell patch clamp technique. HU210 showed a positive allosteric modulating effect in a low micromolar concentration range (EC50: 5.1 ± 2.6μmol/l). Direct activation of glycine receptors was observed at higher concentrations above 100 μmol/l (EC50: 188.7 ± 46.2μmol/l). These in vitro results suggest that strychnine-sensitive glycine receptors may be a target for HU210 mediating some of its anti-inflammatory and anti-nociceptive properties.
© 2009 S. Karger AG, Basel
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