ArticleBMC pharmacology & toxicology2016
Anti-nociceptive and desensitizing effects of olvanil on capsaicin-induced thermal hyperalgesia in the rat.
Article in BMC pharmacology & toxicology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed, 32 citations in OpenAlex.
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- Ononin's Antagonistic Activity towards TRPV1: Insights from Molecular Dynamics and Capsaicin-Evoked Calcium Response in DRG Neurons.Current medicinal chemistry · 2025Article
- Cisplatin Provokes Peripheral Nociception and Neuronal Features of Therapy-Induced Senescence and Calcium Dysregulation in Rats.Neurotoxicity research · 2024Article
- Oral somatosensory alterations and salivary dysfunction in head and neck cancer patients.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2023Article
- The role of adenosine receptor ligands on inflammatory pain: possible modulation of TRPV1 receptor function.Inflammopharmacology · 2023Article
- Article
- TRP channels in COVID-19 disease: Potential targets for prevention and treatment.Chemico-biological interactions · 2021Review
- Fight fire with fire: Neurobiology of capsaicin-induced analgesia for chronic pain.Pharmacology & therapeutics · 2021Review
- CBBritish journal of pharmacology · 2020Article
- Capsaicin and Its Analogues Impede Nocifensive Response of Caenorhabditis elegans to Noxious Heat.Neurochemical research · 2020Article
- Effects of Dual Peroxisome Proliferator-Activated ReceptorsPPAR research · 2019Article
- Topical Treatments for Localized Neuropathic Pain.Current pain and headache reports · 2017Review
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundOlvanil (NE 19550) is a non-pungent synthetic analogue of capsaicin, the natural pungent ingredient of capsicum which activates the transient receptor potential vanilloid type-1 (TRPV1) channel and was developed as a potential analgesic compound. Olvanil has potent anti-hyperalgesic effects in several experimental models of chronic pain. Here we report the inhibitory effects of olvanil on nociceptive processing using cultured dorsal root ganglion (DRG) neurons and compare the effects of capsaicin and olvanil on thermal nociceptive processing in vivo; potential contributions of the cannabinoid CB1 receptor to olvanil's anti-hyperalgesic effects were also investigated.
methodsA hot plate analgesia meter was used to evaluate the anti-nociceptive effects of olvanil on capsaicin-induced thermal hyperalgesia and the role played by CB1 receptors in mediating these effects. Single cell calcium imaging studies of DRG neurons were employed to determine the desensitizing effects of olvanil on capsaicin-evoked calcium responses. Statistical analysis used Student's t test or one way ANOVA followed by Dunnett's post-hoc test as appropriate.
resultsBoth olvanil (100 nM) and capsaicin (100 nM) produced significant increases in intracellular calcium concentrations [Ca(2+)]i in cultured DRG neurons. Olvanil was able to desensitise TRPV1 responses to further capsaicin exposure more effectively than capsaicin. Intraplantar injection of capsaicin (0.1, 0.3 and 1 μg) produced a robust TRPV1-dependant thermal hyperalgesia in rats, whilst olvanil (0.1, 0.3 and 1 μg) produced no hyperalgesia, emphasizing its lack of pungency. The highest dose of olvanil significantly reduced the hyperalgesic effects of capsaicin in vivo. Intraplantar injection of the selective cannabinoid CB1 receptor antagonist rimonabant (1 μg) altered neither capsaicin-induced thermal hyperalgesia nor the desensitizing properties of olvanil, indicating a lack of involvement of CB1 receptors.
conclusionsOlvanil is effective in reducing capsaicin-induced thermal hyperalgesia, probably via directly desensitizing TRPV1 channels in a CB1 receptor-independent fashion. The results presented clearly support the potential for olvanil in the development of new topical analgesic preparations for treating chronic pain conditions while avoiding the unwanted side effects of capsaicin treatments.
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