CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain

Clayton, N.; Marshall, F. H.; Bountra, C.; O'Shaughnessy, C. T.

doi:10.1016/s0304-3959(01)00454-7

Cited by 247Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsIon Channels and Receptors

CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain

Clayton, N., Marshall, F. H., Bountra, C., O'Shaughnessy, C. T.·2002·Pain

DOI 10.1016/s0304-3959(01)00454-7

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Abstract

The cannabinoid agonist, HU210 has been evaluated in vivo in nociceptive and inflammatory pain models in the rat. The ED50 for the anti-nociceptive (increasing mechanical withdrawal threshold) effect was 0.1 mg/kg-1 i.p., and for anti-hypersensitivity and anti-inflammatory activity was 5 g/kg-1 i.p. (in the carrageenan model). The selective CB1 antagonist, AM281 (0.5 microg/kg-1 i.p.) reversed effects of HU210 (10 and 30 microg/kg-1 i.p.) in both nociceptive and inflammatory models of hypersensitivity. The selective CB2 antagonist, SR144528 (1 mg/kg-1 i.p.) antagonised effects of HU210 (30 microg/kg-1 i.p.) in the carrageenan induced inflammatory hypersensitivity. The CB2 agonist, 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(2-(morpholin-4-yl)ethyl)-1H-indole (GW405833) inhibited the hypersensitivity and was anti-inflammatory in vivo. These effects were blocked by SR144528. These findings suggest that CB1 receptors are involved in nociceptive pain and that both CB1 and CB2 receptors are involved in inflammatory hypersensitivity. Future studies will investigate effects on identified inflammatory cells within the inflamed tissue to further elucidate the role of cannabinoid receptors.

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The synthetic cannabinoid agonist HU-210 restores the carrageenan-induced reduction in weight bearing in rats.
“For example, the synthetic cannabinoid agonist HU-210 restores the carrageenan-induced reduction in weight bearing in rats (Clayton et al, 2002;Elmes et al, 2005;Sofia et al, 1973).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Clayton et al, 2002
The selective CB2 receptor agonists GW405833 and JWH133 attenuate edema and restore weight bearing in rat paws injected with carrageenan.
“The selective CB 2 receptor agonists GW405833 and JWH133 attenuate edema and restore weight bearing in rat paws injected with carrageenan (Clayton et al, 2002;Elmes et al, 2005).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Clayton et al, 2002

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Authors: Clayton, N., Marshall, F. H., Bountra, C., & O'Shaughnessy, C. T.
ORCID: Marshall, F. H.
Venue: Pain
Publisher: Ovid Technologies (Wolters Kluwer Health)
Published: 2002-04
Volume: 96
Issue: 3
Pages: 253-260
ISSN: 0304-3959 (ISSN-L)
DOI: 10.1016/s0304-3959(01)00454-7
OpenAlex: W1980122275
Cited by: 247
References: 29
Citations by year: 2026: 8 · 2025: 3 · 2024: 15 · 2023: 11 · 2022: 9 · 2021: 10 · 2020: 12 · 2019: 4 · 2018: 7 · 2017: 11 · 2016: 3 · 2015: 2 · 2014: 7 · 2013: 14 · 2012: 9
FWCI: 7.87
Type: journal article
Language: en
Open access: closed
Locations: Pain (publishedVersion)
PubMed (publishedVersion)
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: CB1 receptor, CB2 receptor, cannabinoid receptors, inflammatory pain, nociceptive pain, HU-210, AM281, SR144528, carrageenan-induced inflammation, antinociceptive effect, anti-inflammatory activity, mechanical withdrawal threshold
MeSH terms: Acute Disease, Animals, Camphanes, Cannabinoids, Carrageenan, Hypersensitivity, Indoles, Male, Morpholines, Nociceptors, Pain, Pyrazoles, Rats, Inbred Strains, Receptors, Drug, Dronabinol, Neurogenic Inflammation, Receptors, Cannabinoid, Receptor, Cannabinoid, CB2, Rats

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CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain

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