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Pharmacology. 2009;83(5):270-4. doi: 10.1159/000209291. Epub 2009 Mar 21.

Modulation of glycine receptor function by the synthetic cannabinoid HU210.

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  • 1Clinic for Anaesthesia and Critical Care Medicine, Hannover Medical School, Hannover, Germany.

Abstract

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 alpha(1 )glycine receptors by using the whole-cell patch clamp technique. HU210 showed a positive allosteric modulating effect in a low micromolar concentration range (EC(50): 5.1 +/- 2.6 micromol/l). Direct activation of glycine receptors was observed at higher concentrations above 100 micromol/l (EC(50): 188.7 +/- 46.2 micromol/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.

Copyright 2009 S. Karger AG, Basel.

PMID:
19307742
[PubMed - indexed for MEDLINE]
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