In:
Pharmacology, S. Karger AG, Vol. 83, No. 5 ( 2009), p. 270-274
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 α 〈 sub 〉 1 〈 /sub 〉 glycine receptors by using the whole-cell patch clamp technique. HU210 showed a positive allosteric modulating effect in a low micromolar concentration range (EC 〈 sub 〉 50 〈 /sub 〉 : 5.1 ± 2.6μmol/l). Direct activation of glycine receptors was observed at higher concentrations above 100 μmol/l (EC 〈 sub 〉 50 〈 /sub 〉 : 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.
Type of Medium:
Online Resource
ISSN:
0031-7012
,
1423-0313
Language:
English
Publisher:
S. Karger AG
Publication Date:
2009
detail.hit.zdb_id:
1483550-2
SSG:
15,3