ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2008
Constitutive activity at the cannabinoid CB1 receptor is required for behavioral response to noxious chemical stimulation of TRPV1: antinociceptive actions of CB1 inverse agonists.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed, 82 citations in OpenAlex.
- The Relationship Between (Endo)cannabinoids, the Microbiome and Melanoma.Pharmacology research & perspectives · 2026Review
- Minor cannabinoids CBD, CBG, CBN, and CBC differentially modulate sensory neuron activation.The Journal of pharmacology and experimental therapeutics · 2026Article
- Minor Cannabinoids CBD, CBG, CBN and CBC differentially modulate sensory neuron activation.bioRxiv : the preprint server for biology · 2025Article
- Anandamide-Mediated Modulation of Nociceptive Transmission at the Spinal Cord Level.Physiological research · 2024Review
- The Endocannabinoid System and Physical Exercise.International journal of molecular sciences · 2023Review
- Peripherally administered cannabinoid receptor 2 (CBBrain research · 2022Article
- Identification of Sodium Transients Through NaFrontiers in cellular neuroscience · 2022Article
- CBBritish journal of pharmacology · 2020Article
- Acetaminophen Relieves Inflammatory Pain through CBThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- Heteromerization Modulates mu Opioid Receptor Functional PropertiesFrontiers in pharmacology · 2018Review
- Potential of Endocannabinoids to Control Bladder Pain.Frontiers in systems neuroscience · 2018Review
- Immunolocalization of cannabinoid receptor type 1 and CB2 cannabinoid receptors, and transient receptor potential vanilloid channels in pterygium.Molecular medicine reports · 2017Article
- Mouse Neuroblastoma CBMethods in enzymology · 2017Article
- Gi-DREADD Expression in Peripheral Nerves Produces Ligand-Dependent Analgesia, as well as Ligand-Independent Functional Changes in Sensory Neurons.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2016Article
- Spatial Distribution of the Cannabinoid Type 1 and Capsaicin Receptors May Contribute to the Complexity of Their Crosstalk.Scientific reports · 2016Article
- Deletion of the murine ATP/UTP receptor P2Y2 alters mechanical and thermal response properties in polymodal cutaneous afferents.Neuroscience · 2016Article
- Transdermal cannabidiol reduces inflammation and pain-related behaviours in a rat model of arthritis.European journal of pain (London, England) · 2016Article
- Capsaicin, Nociception and Pain.Molecules (Basel, Switzerland) · 2016Review
- Regulation of energy balance by a gut-brain axis and involvement of the gut microbiota.Cellular and molecular life sciences : CMLS · 2016Review
- Cannabinoid 1 receptor knockout mice display cold allodynia, but enhanced recovery from spared-nerve injury-induced mechanical hypersensitivity.Molecular pain · 2016Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
Abstract
The potential modulation of TRPV1 nociceptive activity by the CB(1) receptor was investigated here using CB(1) wild-type (WT) and knock-out (KO) mice as well as selective CB(1) inverse agonists. No significant differences were detected in baseline thermal thresholds of ICR, CB(1)WT or CB(1)KO mice. Intraplantar capsaicin produced dose- and time-related paw flinch responses in ICR and CB(1)WT mice and induced plasma extravasation yet minimal responses were seen in CB(1)KO animals with no apparent differences in TRPV1 channel expression. Capsaicin-evoked CGRP release from spinal cord tissue and capsaicin-evoked action potentials on isolated skin-nerve preparation were significantly decreased in CB(1)KO mice. Pretreatment with intraplantar galanin and bradykinin, compounds known to sensitize TRPV1 receptors, restored capsaicin-induced flinching in CB(1)KO mice. The possibility that constitutive activity at the CB(1) receptor is required to maintain the TRPV1 receptor in a "sensitized" state was tested using CB(1) inverse agonists. The CB(1) inverse agonists elicited concentration-related inhibition of capsaicin-induced calcium influx in F-11 cells and produced dose-related inhibition of capsaicin-induced flinching in ICR mice. These data suggest that constitutive activity at the CB(1) receptor maintains the TRPV1 channel in a sensitized state responsive to noxious chemical stimuli. Treatment with CB(1) inverse agonists may promote desensitization of the channel resulting in antinociceptive actions against chemical stimulus modalities. These studies propose possible therapeutic exploitation of a novel mechanism providing pain relief by CB(1) inverse agonists.
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Registered trials
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.