ArticleBritish journal of pharmacology2015
The non-peptide GLP-1 receptor agonist WB4-24 blocks inflammatory nociception by stimulating β-endorphin release from spinal microglia.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers, 1 of them a synthesis that pooled it.
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Who cites it
31 citing papers in PubMed, 1 synthesis or guideline pooled it, 57 citations in OpenAlex.
- Glucagon-like peptide-1 (GLP-1) receptor agonists for headache and pain disorders: a systematic review.The journal of headache and pain · 2024Pooled it
- Effect of liraglutide on expression of inflammatory genes in type 2 diabetes.Scientific reports · 2021Trial
- Glucagon-like Peptide-1 Receptor Agonists and Chronic Pain: Preclinical Antinociceptive Mechanisms, Indirect Metabolic-Functional Effects, and Clinical Considerations-A Narrative Review.Journal of clinical medicine · 2026Review
- GLP-1 receptor agonists in osteoarthritis and psoriatic disease: the missing link between obesity and inflammation?Rheumatology international · 2026Review
- GLP-1R agonists: recent advances, current gaps, and future challenges.Molecular diversity · 2026Review
- New pharmacological agents and emerging therapeutic targets for painful diabetic neuropathy.Frontiers in endocrinology · 2026Review
- Advances in GLP-1 receptor agonists for pain treatment and their future potential.The journal of headache and pain · 2025 · on this mapReview
- Neuropsychiatric adverse events associated with Glucagon-like peptide-1 receptor agonists: a pharmacovigilance analysis of the FDA Adverse Event Reporting System database.European psychiatry : the journal of the Association of European Psychiatrists · 2025Article
- Crotalphine Modulates Microglia M1/M2 Phenotypes and Induces Spinal Analgesia Mediated by Opioid-Cannabinoid Systems.International journal of molecular sciences · 2022Article
- Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- New Advances on Pathophysiology of Diabetes Neuropathy and Pain Management: Potential Role of Melatonin and DPP-4 Inhibitors.Frontiers in pharmacology · 2022Review
- A novel approach to treating opioid use disorders: Dual agonists of glucagon-like peptide-1 receptors and neuropeptide YNeuroscience and biobehavioral reviews · 2021Review
- Teneligliptin Exerts Antinociceptive Effects in Rat Model of Partial Sciatic Nerve Transection Induced Neuropathic Pain.Antioxidants (Basel, Switzerland) · 2021Article
- Molecular insights into differentiated ligand recognition of the human parathyroid hormone receptor 2.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- GLP-1 receptor agonists in the treatment of type 2 diabetes - state-of-the-art.Molecular metabolism · 2021 · on this mapReview
- GLP-1 Receptor Agonists: Beyond Their Pancreatic Effects.Frontiers in endocrinology · 2021Review
- Activation of GLP-1 receptors attenuates oxycodone taking and seeking without compromising the antinociceptive effects of oxycodone in rats.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020Article
- Anti-inflammatory and antinociceptive activities of glucagon-like peptides: evaluation of their actions on serotonergic, nitrergic, and opioidergic systems.Psychopharmacology · 2019Article
- Activation of GPR40 produces mechanical antiallodynia via the spinal glial interleukin-10/β-endorphin pathway.Journal of neuroinflammation · 2019Article
- Effects of glucagon-like peptide 1 receptor agonists on comorbidities in older patients with diabetes mellitus.Therapeutic advances in chronic disease · 2019Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTwo peptide agonists of the glucagon-like peptide-1 (GLP-1) receptor, exenatide and GLP-1 itself, exert anti-hypersensitive effects in neuropathic, cancer and diabetic pain. In this study, we have assessed the anti-allodynic and anti-hyperalgesic effects of the non-peptide agonist WB4-24 in inflammatory nociception and the possible involvement of microglial β-endorphin and pro-inflammatory cytokines. EXPERIMENTAL APPROACH: We used rat models of inflammatory nociception induced by formalin, carrageenan or complete Freund's adjuvant (CFA), to test mechanical allodynia and thermal hyperalgesia. Expression of β-endorphin and pro-inflammatory cytokines was measured using real-time quantitative PCR and fluorescent immunoassays. KEY
resultsWB4-24 displaced the specific binding of exendin (9-39) in microglia. Single intrathecal injection of WB4-24 (0.3, 1, 3, 10, 30 and 100 μg) exerted dose-dependent, specific, anti-hypersensitive effects in acute and chronic inflammatory nociception induced by formalin, carrageenan and CFA, with a maximal inhibition of 60-80%. Spinal WB4-24 was not effective in altering nociceptive pain. Subcutaneous injection of WB4-24 was also antinociceptive in CFA-treated rats. WB4-24 evoked β-endorphin release but did not inhibit expression of pro-inflammatory cytokines in either the spinal cord of CFA-treated rats or cultured microglia stimulated by LPS. WB4-24 anti-allodynia was prevented by a microglial inhibitor, β-endorphin antiserum and a μ-opioid receptor antagonist. CONCLUSIONS AND IMPLICATIONS: Our results suggest that WB4-24 inhibits inflammatory nociception by releasing analgesic β-endorphin rather than inhibiting the expression of proalgesic pro-inflammatory cytokines in spinal microglia, and that the spinal GLP-1 receptor is a potential target molecule for the treatment of pain hypersensitivity including inflammatory nociception.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.