Actions of cannabinoid receptor ligands on rat cultured sensory neurones: implications for antinociception
Abstract
Cannabinoids modulate nociceptive processing in models of acute, inflammatory and neuropathic pain. We have investigated the location and function of cannabinoid receptors on cultured neonatal dorsal root ganglion (DRG) neurones and F-11 cells, a dorsal root ganglionxneuroblastoma hybridoma which displays several of the features of authentic DRG neurones. CB(1) receptor immunolabelling was observed on the cell bodies and as fine puncta on processes of both cultured DRG neurones and F-11 cells. Additionally, fluorescence-activated cell sorting (FACS) analysis provided evidence that both CB(1) and CB(2) receptors are expressed on populations of cells within the cultured DRG and F-11 cells. The cannabinoid receptor agonist (+)-WIN55212 (10 and 100 nM) inhibited the mean voltage-activated Ca(2+) current in DRG neurones by 21% and 30%, respectively. The isomer, (-)-WIN55212 (10 and 100 nM) produced significantly less inhibition of 6% and 10% respectively. The CB(1) selective receptor antagonist SR141716A (100 nM) enhanced the peak high voltage-activated Ca(2+) current by 24% and simultaneous application of SR141716A (100 nM) and (+)-WIN55212 (100 nM) resulted in a significant attenuation of the inhibition obtained with (+)-WIN55212 alone. These data give functional evidence for the hypothesis that the analgesic actions of cannabinoids may be mediated by presynaptic inhibition of transmitter release in sensory neurones.
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CB2 receptor protein has been reported in the dorsal root ganglia, brainstem, thalamus, periaqueductal gray, and cerebellum of naive rats.
“CB2 receptor protein has been reported in the DRG,13 brainstem,14 thalamus,15 PAG,15 and cerebellum15, 16 of naive rats.”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [13]
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- Authors
- Ross, R. A., Coutts, A. A., McFarlane, S. M., Anavi-Goffer, S., Irving, A. J., Pertwee, R. G., MacEwan, D. J., & Scott, R. H.
- Affiliations
- University of Aberdeen (GB)
- Corresponding author
- Ross, Ruth A
- Venue
- Neuropharmacology
- Publisher
- Elsevier BV
- Published
- 2001-01
- Volume
- 40
- Issue
- 2
- Pages
- 221-232
- ISSN
- 0028-3908 (ISSN-L)
- OpenAlex
- W2028253575
- Cited by
- 172
- References
- 37
- Citations by year
- 2025: 1 · 2023: 2 · 2021: 5 · 2020: 4 · 2019: 3 · 2018: 2 · 2017: 4 · 2016: 1 · 2015: 1 · 2014: 6 · 2013: 5 · 2012: 8
- FWCI
- 10.24
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Neuropharmacology (publishedVersion)
- PubMed (publishedVersion)
- UEA Digital Repository (University of East Anglia) (submittedVersion)
- Funders
- Sanofi
- Wellcome Trust
- Topics
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- cannabinoid receptors, CB1 receptor, CB2 receptor, dorsal root ganglion neurons, sensory neurons, antinociception, SR141716A, voltage-activated calcium currents, presynaptic inhibition, nociception
- MeSH terms
- Cyclic AMP, Animals, Animals, Newborn, Calcium Channel Blockers, Cannabinoids, Cells, Cultured, Fluorescence, Colforsin, Ganglia, Spinal, Immunohistochemistry, Ligands, Morpholines, Naphthalenes, Neurons, Afferent, Receptors, Drug, Calcium Channels, Ion Channel Gating, Rats, Wistar, Patch-Clamp Techniques, Receptors, Cannabinoid, Receptor, Cannabinoid, CB2, Benzoxazines, Rats
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