Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Br J Pharmacol
2001 Mar 01;1325:1084-94. doi: 10.1038/sj.bjp.0703918.
Show Gene links
Show Anatomy links
Pharmacological differences between the human and rat vanilloid receptor 1 (VR1).
McIntyre P, McLatchie LM, Chambers A, Phillips E, Clarke M, Savidge J, Toms C, Peacock M, Shah K, Winter J, Weerasakera N, Webb M, Rang HP, Bevan S, James IF.
???displayArticle.abstract???
Vanilloid receptors (VR1) were cloned from human and rat dorsal root ganglion libraries and expressed in Xenopus oocytes or Chinese Hamster Ovary (CHO) cells. Both rat and human VR1 formed ligand gated channels that were activated by capsaicin with similar EC(50) values. Capsaicin had a lower potency on both channels, when measured electrophysiologically in oocytes compared to CHO cells (oocytes: rat=1.90+/-0.20 microM; human=1.90+/-0.30 microM: CHO cells: rat=0.20+/-0.06 microM; human=0.19+/-0.08 microM). In CHO cell lines co-expressing either rat or human VR1 and the calcium sensitive, luminescent protein, aequorin, the EC(50) values for capsaicin-induced responses were similar in both cell lines (rat=0.35+/-0.06 microM, human=0.53+/-0.03 microM). The threshold for activation by acidic solutions was lower for human VR1 channels than that for rat VR1 (EC(50) pH 5.49+/-0.04 and pH 5.78+/-0.09, respectively). The threshold for heat activation was identical (42 degrees C) for rat and human VR1. PPAHV was an agonist at rat VR1 (EC(50) between 3 and 10 microM) but was virtually inactive at the human VR1 (EC(50)>10 microM). Capsazepine and ruthenium red were both more potent at blocking the capsaicin response of human VR1 than rat VR1. Capsazepine blocked the human but not the rat VR1 response to low pH. Capsazepine was also more effective at inhibiting the noxious heat response of human than of rat VR1.
Appendino,
Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of cooperativity.
1996, Pubmed
Appendino,
Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of cooperativity.
1996,
Pubmed Aviv,
Purification of biologically active globin messenger RNA by chromatography on oligothymidylic acid-cellulose.
1972,
Pubmed Baumann,
Responses of adult human dorsal root ganglion neurons in culture to capsaicin and low pH.
1996,
Pubmed Bevan,
Sensory neuron-specific actions of capsaicin: mechanisms and applications.
1990,
Pubmed Bevan,
Nerve growth factor (NGF) differentially regulates the chemosensitivity of adult rat cultured sensory neurons.
1995,
Pubmed Bevan,
Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin.
1992,
Pubmed Brini,
Transfected aequorin in the measurement of cytosolic Ca2+ concentration ([Ca2+]c). A critical evaluation.
1995,
Pubmed Caterina,
The capsaicin receptor: a heat-activated ion channel in the pain pathway.
1997,
Pubmed
,
Xenbase Caterina,
A capsaicin-receptor homologue with a high threshold for noxious heat.
1999,
Pubmed
,
Xenbase Caterina,
Impaired nociception and pain sensation in mice lacking the capsaicin receptor.
2000,
Pubmed Chomczynski,
Single-step method of RNA isolation by acid guanidinium thiocyanate-phenol-chloroform extraction.
1987,
Pubmed Davis,
Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia.
2000,
Pubmed Docherty,
Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture.
1997,
Pubmed Hayes,
Cloning and functional expression of a human orthologue of rat vanilloid receptor-1.
2000,
Pubmed
,
Xenbase Helliwell,
Capsaicin sensitivity is associated with the expression of the vanilloid (capsaicin) receptor (VR1) mRNA in adult rat sensory ganglia.
1998,
Pubmed Hwang,
Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances.
2000,
Pubmed Jerman,
Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology.
2000,
Pubmed Jordt,
Acid potentiation of the capsaicin receptor determined by a key extracellular site.
2000,
Pubmed Jung,
Capsaicin binds to the intracellular domain of the capsaicin-activated ion channel.
1999,
Pubmed Kirschstein,
Inhibition of rapid heat responses in nociceptive primary sensory neurons of rats by vanilloid receptor antagonists.
1999,
Pubmed Kress,
An interaction of inflammatory mediators and protons in small diameter dorsal root ganglion neurons of the rat.
1997,
Pubmed Liu,
A non-pungent resiniferatoxin analogue, phorbol 12-phenylacetate 13 acetate 20-homovanillate, reveals vanilloid receptor subtypes on rat trigeminal ganglion neurons.
1998,
Pubmed Liu,
Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia.
1997,
Pubmed Liu,
Similarities and differences in the currents activated by capsaicin, piperine, and zingerone in rat trigeminal ganglion cells.
1996,
Pubmed Nagy,
Similarities and differences between the responses of rat sensory neurons to noxious heat and capsaicin.
1999,
Pubmed Savidge,
Comparison of intracellular calcium signals evoked by heat and capsaicin in cultured rat dorsal root ganglion neurons and in a cell line expressing the rat vanilloid receptor, VR1.
2001,
Pubmed Shu,
Nerve growth factor acutely sensitizes the response of adult rat sensory neurons to capsaicin.
1999,
Pubmed Smart,
The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1).
2000,
Pubmed Szallasi,
Resiniferatoxin-type phorboid vanilloids display capsaicin-like selectivity at native vanilloid receptors on rat DRG neurons and at the cloned vanilloid receptor VR1.
1999,
Pubmed Tominaga,
The cloned capsaicin receptor integrates multiple pain-producing stimuli.
1998,
Pubmed
,
Xenbase Vyklický,
Inflammatory mediators at acidic pH activate capsaicin receptors in cultured sensory neurons from newborn rats.
1998,
Pubmed Walpole,
Similarities and differences in the structure-activity relationships of capsaicin and resiniferatoxin analogues.
1996,
Pubmed Zygmunt,
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide.
1999,
Pubmed
,
Xenbase
