Effect of the cannabinoid CB1 receptor antagonist, SR141716, on nociceptive response and nerve demyelination in rodents with chronic constriction injury of the sciatic nerve

Costa, Barbara; Trovato, Anna Elisa; Colleoni, Mariapia; Giagnoni, Gabriella; Zarini, Elena; Croci, Tiziano

doi:10.1016/j.pain.2005.03.043

Cited by 104Pain Mechanisms and TreatmentsCannabis and Cannabinoid ResearchPain Management and Treatment

Effect of the cannabinoid CB1 receptor antagonist, SR141716, on nociceptive response and nerve demyelination in rodents with chronic constriction injury of the sciatic nerve

Costa, Barbara, Trovato, Anna Elisa, Colleoni, Mariapia, Giagnoni, Gabriella, Zarini, Elena, Croci, Tiziano·2005·Pain

DOI 10.1016/j.pain.2005.03.043

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Abstract

Many reports have shown the efficacy of cannabinoid agonists in chronic pain, whereas no report exists concerning the potential effect of cannabinoid antagonists following prolonged treatment. We tested the effects of repeated administration of the selective cannabinoid receptor type 1 (CB1) antagonist, SR141716 (rimonabant), in rats with chronic constriction injury of the sciatic nerve (CCI), an animal model of neuropathic pain. The repeated oral administration of SR141716 (1, 3 and 10 mg/kg, once a day for 1 week, from day 7 after the injury) dose dependently attenuated both thermal and mechanical hyperalgesia. A similar effect was observed in CCI wild-type mice, whereas SR141716 was unable to elicit pain relief in CB1 knockout mice, suggesting CB1 receptors involvement in the SR141716-induced antihyperalgesia. The antihyperalgesic activity of SR141716 was associated with a significant reduction of several pro-inflammatory and pro-nociceptive mediators such as tumor necrosis factor alpha (TNFalpha), prostaglandin-E2 (PGE2), lipoperoxide and nitric oxide (NO) levels. The histological analysis of sciatic nerve sections showed a marked degeneration of myelinated fibers in CCI rats, which was substantially reduced after repeated administration of SR141716. This suggests that the compound may favour myelin repair and consequently promote long-lasting functional recovery. This was confirmed by the maintenance of recovery for at least four weeks after treatment discontinuation. In conclusion, the present findings suggest that SR141716 is effective not only in alleviating neuropathic pain but also in favouring the nerve myelin repair.

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SR141716 administered chronically suppresses thermal and mechanical hyperalgesia in both rats and CB1+/+ mice, while failing to produce an effect in CB1-/- mice.
“However, SR141716 (p.o.), administered chronically, suppresses thermal and mechanical hyperalgesia in both rats and CB1+/+ mice, while failing to produce an effect in CB1-/- mice. 43”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [43]

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Authors: Costa, B., Trovato, A. E., Colleoni, M., Giagnoni, G., Zarini, E., & Croci, T.
Affiliations: University of Milano-Bicocca (IT)
University of Milan (IT)
Sanofi (Italy) (IT)
Corresponding author: Costa, Barbara
ORCID: Costa, Barbara
Venue: Pain
Publisher: Ovid Technologies (Wolters Kluwer Health)
Published: 2005-07
Volume: 116
Issue: 1
Pages: 52-61
ISSN: 0304-3959 (ISSN-L)
DOI: 10.1016/j.pain.2005.03.043
OpenAlex: W2063734790
Cited by: 104
References: 41
Citations by year: 2024: 4 · 2023: 1 · 2022: 3 · 2021: 7 · 2020: 4 · 2019: 2 · 2018: 6 · 2017: 6 · 2016: 7 · 2015: 3 · 2014: 7 · 2013: 7 · 2012: 6
FWCI: 4.99
Type: journal article
Language: en
Open access: closed
Locations: Pain (publishedVersion)
PubMed (publishedVersion)
BOA (University of Milano-Bicocca) (submittedVersion)
Topics: Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Anesthesiology and Pain Medicine › Pain Management and Treatment
Keywords: SR141716, rimonabant, CB1 receptor antagonist, cannabinoid receptors, neuropathic pain, chronic constriction injury, sciatic nerve, nerve demyelination, remyelination, antihyperalgesia, TNF-α, prostaglandin E2, nitric oxide, lipid peroxidation, CB1 knockout mice, functional recovery
MeSH terms: Rimonabant, Analysis of Variance, Animals, Constriction, Demyelinating Diseases, Enzyme-Linked Immunosorbent Assay, Lipid Peroxides, Male, Nerve Tissue Proteins, Nitrates, Nitrites, Pain, Pain Measurement, Piperidines, Pyrazoles, Reaction Time, Sciatic Nerve, Staining and Labeling, Tumor Necrosis Factor-alpha, Blotting, Western, Dinoprostone, Rats, Wistar, Mice, Knockout, Nitric Oxide Synthase, Sciatic Neuropathy, Receptors, Cannabinoid, Mice, Rats, Nitric Oxide Synthase Type II, Nitric Oxide Synthase Type I, Cannabinoid Receptor Antagonists

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Effect of the cannabinoid CB1 receptor antagonist, SR141716, on nociceptive response and nerve demyelination in rodents with chronic constriction injury of the sciatic nerve

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