ArticleBritish journal of pharmacology2018
Antinociceptive effect of two novel transient receptor potential melastatin 8 antagonists in acute and chronic pain models in rat.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 47 citations in OpenAlex.
- Somatosensory Functions of Melastatin Transient-Receptor Potential Channels in the Teeth: Molecular Basis for Thermal Dentine Hypersensitivity.Dentistry journal · 2026Review
- Osteoarthritis: molecular pathogenesis and potential therapeutic options.Signal transduction and targeted therapy · 2026Review
- Corneal Sensory Receptors and Pharmacological Therapies to Modulate Ocular Pain.International journal of molecular sciences · 2025Review
- Subcutaneous administration of a novel TRPM8 antagonist reverses cold hypersensitivity while attenuating the drop in core body temperature.British journal of pharmacology · 2024Article
- Mechanisms of sensory adaptation and inhibition of the cold and menthol receptor TRPM8.Science advances · 2024Article
- Transient Receptor Potential Channels: Multiple Modulators of Peripheral Neuropathic Pain in Several Rodent Models.Neurochemical research · 2024Review
- Ion channels in cancer-induced bone pain: from molecular mechanisms to clinical applications.Frontiers in molecular neuroscience · 2023Review
- General anaesthesia-related complications of gut motility with a focus on cholinergic mechanisms, TRP channels and visceral pain.Frontiers in physiology · 2023Article
- Transient Receptor Potential Channels: Important Players in Ocular Pain and Dry Eye Disease.Pharmaceutics · 2022Review
- β-Lactam TRPM8 Antagonist RGM8-51 Displays Antinociceptive Activity in Different Animal Models.International journal of molecular sciences · 2022Article
- Dexmedetomidine Alleviates Neuropathic Pain via the TRPC6-p38 MAPK Pathway in the Dorsal Root Ganglia of Rats.Journal of pain research · 2022Article
- Involvement of Opioid System and TRPM8/TRPA1 Channels in the Antinociceptive Effect ofBiomolecules · 2021Article
- TRPV4 and TRPM8 as putative targets for chronic low back pain alleviation.Pflugers Archiv : European journal of physiology · 2021Article
- Topical TRPM8 Agonist for Relieving Neuropathic Ocular Pain in Patients with Dry Eye: A Pilot Study.Journal of clinical medicine · 2021Article
- Oxaliplatin Depolarizes the IB4Frontiers in molecular neuroscience · 2021Article
- Heat Emitting Damage in Skin: A Thermal Pathway for Mechanical Algesia.Frontiers in neuroscience · 2021Article
- TRPM Channels in Human Diseases.Cells · 2020Review
- TRPM8: A Therapeutic Target for Neuroinflammatory Symptoms Induced by Severe Dry Eye Disease.International journal of molecular sciences · 2020Article
- Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.Journal of medicinal chemistry · 2020Article
- Structure-Based Design of Novel Biphenyl Amide Antagonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 8 Channels with Potential Implications in the Treatment of Sensory Neuropathies.ACS chemical neuroscience · 2020Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTransient receptor potential (TRP) channels are a superfamily of non-selective cation permeable channels involved in peripheral sensory signalling. Animal studies have shown that several TRPs are important players in pain modulation. Among them, the TRP melastatin 8 (TRPM8) has elicited more interest for its controversial role in nociception. This channel, expressed by a subpopulation of sensory neurons in dorsal root ganglia (DRG) and trigeminal ganglia (TG), is activated by cold temperatures and cooling agents. In experimental neuropathic pain models, an up-regulation of this receptor in DRG and TG has been observed, suggesting a key role for TRPM8 in the development and maintenance of pain. Consistent with this hypothesis, TRPM8 knockout mice are less responsive to pain stimuli. EXPERIMENTAL APPROACH: In this study, the therapeutic potential and efficacy of two novel TRPM8 antagonists, DFL23693 and DFL23448, were tested. KEY
resultsTwo potent and selective TRPM8 antagonists with distinct pharmacokinetic profiles, DFL23693 and DFL23448, have been fully characterized in vitro. In vivo studies in well-established models, namely, the wet-dog shaking test and changes in body temperature, confirmed their ability to block the TRPM8 channel. Finally, TRPM8 blockage resulted in a significant antinociceptive effect in formalin-induced orofacial pain and in chronic constriction injury-induced neuropathic pain, confirming an important role for this channel in pain perception. CONCLUSION AND IMPLICATIONS: Our findings, in agreement with previous literature, encourage further studies for a better comprehension of the therapeutic potential of TRPM8 blockers as novel agents for pain management.
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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.