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Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 2013 Nov 15; Vol. 720 (1-3), pp. 310-9. Date of Electronic Publication: 2013 Oct 18. - Publication Year :
- 2013
-
Abstract
- The effects of cannabidiol (CBD), a non-psychoactive ingredient of cannabis plant, on the function of the cloned α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes were tested using the two-electrode voltage-clamp technique. CBD reversibly inhibited ACh (100 μM)-induced currents with an IC50 value of 11.3 µM. Other phytocannabinoids such as cannabinol and Δ(9)-tetrahydrocannabinol did not affect ACh-induced currents. CBD inhibition was not altered by pertussis toxin treatment. In addition, CBD did not change GTP-γ-S binding to the membranes of oocytes injected with α7 nACh receptor cRNA. The effect of CBD was not dependent on the membrane potential. CBD (10 µM) did not affect the activity of endogenous Ca(2+)-dependent Cl(-) channels, since the extent of inhibition by CBD was unaltered by intracellular injection of the Ca(2+) chelator BAPTA and perfusion with Ca(2+)-free bathing solution containing 2mM Ba(2+). Inhibition by CBD was not reversed by increasing ACh concentrations. Furthermore, specific binding of [(125)I] α-bungarotoxin was not inhibited by CBD (10 µM) in oocytes membranes. Using whole cell patch clamp technique in CA1 stratum radiatum interneurons of rat hippocampal slices, currents induced by choline, a selective-agonist of α7-receptor induced currents were also recoded. Bath application of CBD (10 µM) for 10 min caused a significant inhibition of choline induced currents. Finally, in hippocampal slices, [(3)H] norepinephrine release evoked by nicotine (30 µM) was also inhibited by 10 µM CBD. Our results indicate that CBD inhibits the function of the α7-nACh receptor.<br /> (© 2013 Published by Elsevier B.V.)
- Subjects :
- Acetylcholine pharmacology
Animals
Bungarotoxins pharmacology
Choline pharmacology
Guanosine 5'-O-(3-Thiotriphosphate) pharmacology
Hippocampus drug effects
Hippocampus physiology
Humans
Male
Nicotine pharmacology
Nicotinic Antagonists pharmacology
Norepinephrine metabolism
Oocytes metabolism
Radioligand Assay
Rats
Rats, Sprague-Dawley
Xenopus laevis
alpha7 Nicotinic Acetylcholine Receptor agonists
alpha7 Nicotinic Acetylcholine Receptor metabolism
Cannabidiol pharmacology
alpha7 Nicotinic Acetylcholine Receptor antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0712
- Volume :
- 720
- Issue :
- 1-3
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 24140434
- Full Text :
- https://doi.org/10.1016/j.ejphar.2013.10.011