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Original Paper

Modulation of Glycine Receptor Function by the Synthetic Cannabinoid HU210

Demir 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

Author affiliations

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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Pharmacology 2009;83:270–274

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: January 20, 2009
Accepted: January 28, 2009
Published online: March 21, 2009
Issue release date: May 2009

Number of Print Pages: 5
Number of Figures: 2
Number of Tables: 0

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: https://www.karger.com/PHA

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 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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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: January 20, 2009
Accepted: January 28, 2009
Published online: March 21, 2009
Issue release date: May 2009

Number of Print Pages: 5
Number of Figures: 2
Number of Tables: 0

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: https://www.karger.com/PHA


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