ArticleBritish journal of pharmacology2000
Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 116 citations in OpenAlex.
- The 18th international workshop on osteoarthritis imaging. Structure and pain: Where are we today?Osteoarthritis imaging · 2025Review
- Neuronal cell lines as model dorsal root ganglion neurons: A transcriptomic comparison.Molecular pain · 2016Article
- Increased function of the TRPV1 channel in small sensory neurons after local inflammation or in vitro exposure to the pro-inflammatory cytokine GRO/KC.Neuroscience bulletin · 2012Article
- Capsaicin-induced vasodilatation in human nasal vasculature is mediated by modulation of cyclooxygenase-2 activity and abrogated by sulprostone.Naunyn-Schmiedeberg's archives of pharmacology · 2011Article
- A pathogenic C terminus-truncated polycystin-2 mutant enhances receptor-activated Ca2+ entry via association with TRPC3 and TRPC7.The Journal of biological chemistry · 2009Article
- Behavioral and electrophysiological evidence for the differential functions of TRPV1 at early and late stages of chronic inflammatory nociception in rats.Neurochemical research · 2008Article
- TRPA1 mediates the noxious effects of natural sesquiterpene deterrents.The Journal of biological chemistry · 2008Article
- A yeast genetic screen reveals a critical role for the pore helix domain in TRP channel gating.Neuron · 2008Article
- Thymol and related alkyl phenols activate the hTRPA1 channel.British journal of pharmacology · 2008Article
- Facilitation and inhibition by capsaicin of cholinergic neurotransmission in the guinea-pig small intestine.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- The effects of Delta9-tetrahydrocannabinol in rat mesenteric vasculature, and its interactions with the endocannabinoid anandamide.British journal of pharmacology · 2005Article
- Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1).British journal of pharmacology · 2005Article
- Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.British journal of pharmacology · 2004Article
- Capsazepine protects against neuronal injury caused by oxygen glucose deprivation by inhibiting I(h).The Journal of neuroscience : the official journal of the Society for Neuroscience · 2003Article
- Activation of vanilloid receptor type I in the endoplasmic reticulum fails to activate store-operated Ca2+ entry.The Biochemical journal · 2003Article
- Capsaicinoids cause inflammation and epithelial cell death through activation of vanilloid receptors.Toxicological sciences : an official journal of the Society of Toxicology · 2003Article
- Comparison of human recombinant adenosine A2B receptor function assessed by Fluo-3-AM fluorometry and microphysiometry.British journal of pharmacology · 2003Article
- Activation of vanilloid receptor 1 by resiniferatoxin mobilizes calcium from inositol 1,4,5-trisphosphate-sensitive stores.British journal of pharmacology · 2003Article
- Respiratory actions of vanilloid receptor agonists in the nucleus of the solitary tract: comparison of resiniferatoxin with non-pungent agents and anandamide.British journal of pharmacology · 2002Article
- Anandamide is a partial agonist at native vanilloid receptors in acutely isolated mouse trigeminal sensory neurons.British journal of pharmacology · 2002Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The vanilloid receptor (VR1) is a ligand-gated ion channel, which plays an important role in nociceptive processing. Therefore, a pharmacological characterization of the recently cloned rat VR1 (rVR1) was undertaken. HEK293 cells stable expressing rVR1 (rVR1-HEK293) were loaded with Fluo-3AM and then incubated at 25 degrees C for 30 min with or without various antagonists or signal transduction modifying agents. Then intracellular calcium concentrations ([Ca(2+)](i)) were monitored using FLIPR, before and after the addition of various agonists. The rank order of potency of agonists (resiniferatoxin (RTX)>capsaicin>olvanil>PPAHV) was as expected, and all were full agonists. The potencies of capsaicin and olvanil, but not RTX or PPAHV, were enhanced at pH 6.4 (pEC(50) values of 7.47+/-0.06, 7.16+/-0.06, 8.19+/-0.06 and 6.02+/-0.03 respectively at pH 7.4 vs 7.71+/-0.05, 7.58+/-0.14, 8.10+/-0.05 and 6.04+/-0.08 at pH 6.4). Capsazepine, isovelleral and ruthenium red all inhibited the capsaicin (100 nM)-induced Ca(2+) response in rVR1-HEK293 cells, with pK(B) values of 7.52+/-0.08, 6.92+/-0.11 and 8.09+/-0.12 respectively (n=6 each). The response to RTX and olvanil were also inhibited by these compounds. None displayed any agonist-like activity. The removal of extracellular Ca(2+) abolished, whilst inhibition of protein kinase C with chelerythrine chloride (10 microM) partially (approximately 20%) inhibited, the capsaicin (10 microM)-induced Ca(2+) response. However, tetrodotoxin (3 microM), nimodipine (10 microM), omega-GVIA conotoxin (1 microM), thapsigargin (1 microM), U73122 (3 microM) or H-89 (3 microM) had no effect on the capsaicin (100 nM)-induced response. In conclusion, the recombinant rVR1 stably expressed in HEK293 cells acts as a ligand-gated Ca(2+) channel with the appropriate agonist and antagonist pharmacology, and therefore is a suitable model for studying the effects of drugs at this receptor.
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