ArticleNeuropharmacology2011
Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons.
Article in Neuropharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 41 citations in OpenAlex.
- Investigation of the cytotoxicity induced by cannabinoids on human ovarian carcinoma cells.Pharmacology research & perspectives · 2023Article
- Exploring the Therapeutic Potential of Cannabinoid Receptor Antagonists in Inflammation, Diabetes Mellitus, and Obesity.Biomedicines · 2023Review
- Activation of Peripheral Cannabinoid Receptors Synergizes the Effect of Systemic Ibuprofen in a Pain Model in Rat.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Intersections in Neuropsychiatric and Metabolic Disorders: Possible Role of TRPA1 Channels.Frontiers in endocrinology · 2021Review
- CBBritish journal of pharmacology · 2020Article
- Cannabinoids Modulate Neuronal Activity and Cancer by CB1 and CB2 Receptor-Independent Mechanisms.Frontiers in pharmacology · 2017Review
- The CBCellular and molecular life sciences : CMLS · 2016Review
- Cannabinoids increase mechanosensitivity of trigeminal ganglion neurons innervating the inner walls of rat anterior chambers via activation of TRPA1.Journal of Huazhong University of Science and Technology. Medical sciences = Hua zhong ke ji da xue xue bao. Yi xue Ying De wen ban = Huazhong keji daxue xuebao. Yixue Yingdewen ban · 2016Article
- Cannabinoid Receptors Are Overexpressed in CLL but of Limited Potential for Therapeutic Exploitation.PloS one · 2016Article
- The synthetic cannabinoid WIN55,212-2 mesylate decreases the production of inflammatory mediators in rheumatoid arthritis synovial fibroblasts by activating CB2, TRPV1, TRPA1 and yet unidentified receptor targets.Journal of inflammation (London, England) · 2016Article
- Cannabinoid-based drugs targeting CB1 and TRPV1, the sympathetic nervous system, and arthritis.Arthritis research & therapy · 2015Review
- TRP channel cannabinoid receptors in skin sensation, homeostasis, and inflammation.ACS chemical neuroscience · 2014Review
- Cannabinoid 1 and transient receptor potential vanilloid 1 receptors discretely modulate evoked glutamate separately from spontaneous glutamate transmission.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- Mechanisms of transient signaling via short and long prolactin receptor isoforms in female and male sensory neurons.The Journal of biological chemistry · 2013Article
- The transient receptor potential channel TRPA1: from gene to pathophysiology.Pflugers Archiv : European journal of physiology · 2012Review
- Differences in peripheral endocannabinoid modulation of scratching behavior in facial vs. spinally-innervated skin.Neuropharmacology · 2012Article
- Receptor and channel heteromers as pain targets.Pharmaceuticals (Basel, Switzerland) · 2012Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Cannabinoid receptor antagonists have been utilized extensively in vivo as well as in vitro, but their selectivity has not been fully examined. We investigated activation of sensory neurons by two cannabinoid antagonists - AM251 and AM630. AM251 and AM630 activated trigeminal (TG) sensory neurons in a concentration-dependent fashion (threshold 1 μM). AM251 and AM630 responses are mediated by the TRPA1 channel in a majority (90-95%) of small-to-medium TG sensory neurons. AM630 (1-100 μM), but not AM251, was a significantly more potent agonist in cells co-expressing both TRPA1 and TRPV1 channels. We next evaluated AM630 and AM251 effects on TRPV1- and TRPA1-mediated responses in TG neurons. Capsaicin (CAP) effects were inhibited by pre-treatment with AM630, but not AM251. Mustard oil (MO) and WIN55,212-2 (WIN) TRPA1 mediated responses were also inhibited by pre-treatment with AM630, but not AM251 (25 uM each). Co-treatment of neurons with WIN and either AM630 or AM251 had opposite effects: AM630 sensitized WIN responses, whereas AM251 inhibited WIN responses. WIN-induced inhibition of CAP responses in sensory neurons was reversed by AM630 pre-treatment and AM251 co-treatment (25 μM each), as these conditions inhibit WIN responses. Hindpaw injections of AM630 and AM251 did not produce nocifensive behaviors. However, both compounds modulated CAP-induced thermal hyperalgesia in wild-type mice and rats, but not TRPA1 null-mutant mice. AMs also partially regulate WIN inhibition of CAP-induced thermal hyperalgesia in a TRPA1-dependent fashion. In summary, these findings demonstrate alternative targets for the cannabinoid antagonists, AM251 and AM630, in peripheral antihyperalgesia which involve certain TRP channels.
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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.