In:
Pharmacology, S. Karger AG, Vol. 83, No. 4 ( 2009), p. 217-222
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. Cannabidiol is a nonpsychotropic plant constituent of 〈 i 〉 Cannabis sativa 〈 /i 〉 . 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 α 〈 sub 〉 1 〈 /sub 〉 and α 〈 sub 〉 1 〈 /sub 〉 β glycine receptors by using the whole-cell patch clamp technique. Cannabidiol showed a positive allosteric modulating effect in a low micromolar concentration range (EC 〈 sub 〉 50 〈 /sub 〉 values: α 〈 sub 〉 1 〈 /sub 〉 = 12.3 ± 3.8 μmol/l and α 〈 sub 〉 1 〈 /sub 〉 β = 18.1 ± 6.2 μmol/l). Direct activation of glycine receptors was observed at higher concentrations above 100 μmol/l (EC 〈 sub 〉 50 〈 /sub 〉 values: α 〈 sub 〉 1 〈 /sub 〉 = 132.4 ± 12.3 μmol/l and α 〈 sub 〉 1 〈 /sub 〉 β = 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.
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
