(Q36506375)

14 August 2017

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title

Small molecule vanilloid TRPV1 receptor antagonists approaching drug status: can they live up to the expectations? (English)

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14 August 2017

Arpad Szallasi

1

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14 August 2017

language of work or name

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14 June 2006

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Naunyn-Schmiedeberg's Archives of Pharmacology

14 August 2017

published in

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14 August 2017

volume

373

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14 August 2017

issue

4

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14 August 2017

page(s)

273-286

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A hot new twist to hair biology: involvement of vanilloid receptor-1 (VR1/TRPV1) signaling in human hair growth control

14 August 2017

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Influences of aging on taste perception and oral somatic sensation

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Early painful diabetic neuropathy is associated with differential changes in the expression and function of vanilloid receptor 1.

21 January 2018

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Involvement of serum retinoids and Leiden mutation in patients with esophageal, gastric, liver, pancreatic, and colorectal cancers in Hungary

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More than spice: capsaicin in hot chili peppers makes tumor cells commit suicide

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Resiniferatoxin binding to vanilloid receptors in guinea pig and human airways

21 January 2018

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Current perspectives on the therapeutic utility of VR1 antagonists

21 January 2018

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https://api.crossref.org/works/10.1007%2FS00210-006-0072-3

Sensitization and translocation of TRPV1 by insulin and IGF-I.

21 January 2018

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12 December 2020

NGF and GDNF differentially regulate TRPV1 expression that contributes to development of inflammatory thermal hyperalgesia.

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12 December 2020

A modular PIP2 binding site as a determinant of capsaicin receptor sensitivity

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12 December 2020

Local inflammation increases vanilloid receptor 1 expression within distinct subgroups of DRG neurons

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12 December 2020

Peptide immunoreactivity and ultrastructure of rat urinary bladder nerve fibers after topical desensitization by capsaicin or resiniferatoxin

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12 December 2020

Peripheral inflammation selectively increases TRPV1 function in IB4-positive sensory neurons from adult mouse

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12 December 2020

Expression and characterization of the intracellular vanilloid receptor (TRPV1) in bronchi from patients with chronic cough

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12 December 2020

TRP ion channels in the nervous system.

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12 December 2020

Tumor initiators and promoters in the induction of Epstein—Barr virus

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12 December 2020

Structure-function analysis of TRPV channels

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12 December 2020

Participation of vanilloid/capsaicin receptors, calcitonin-gene-related peptide and substance P in gastric protection of omeprazole and omeprazole-like compounds

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12 December 2020

Molecular mechanisms of nociception

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12 December 2020

Peripheral capsaicin receptors increase in the inflamed rat hindpaw: a possible mechanism for peripheral sensitization

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12 December 2020

Arachidonyl ethanolamide induces apoptosis of uterine cervix cancer cells via aberrantly expressed vanilloid receptor-1.

1 reference

12 December 2020

The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain.

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12 December 2020

Altered urinary bladder function in mice lacking the vanilloid receptor TRPV1

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12 December 2020

Functional vanilloid receptors in cultured normal human epidermal keratinocytes

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12 December 2020

Forty years in capsaicin research for sensory pharmacology and physiology

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12 December 2020

Immunohistochemical distribution of vanilloid receptor, calcitonin-gene related peptide and substance P in gastrointestinal mucosa of patients with different gastrointestinal disorders

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12 December 2020

Molecular mechanisms of neuropathic pain-phenotypic switch and initiation mechanisms

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12 December 2020

Pharmacology of inhaled capsaicin in humans

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12 December 2020

Expression of vanilloid receptor-1 in epithelial cells of human antral gastric mucosa

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12 December 2020

A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats

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12 December 2020

Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?

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12 December 2020

Transient receptor potential vanilloid 4 is essential in chemotherapy-induced neuropathic pain in the rat.

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12 December 2020

Heteromerization and colocalization of TrpV1 and TrpV2 in mammalian cell lines and rat dorsal root ganglia

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12 December 2020

Functional recovery from desensitization of vanilloid receptor TRPV1 requires resynthesis of phosphatidylinositol 4,5-bisphosphate.

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12 December 2020

Treatment of trigeminal ganglion neurons in vitro with NGF, GDNF or BDNF: effects on neuronal survival, neurochemical properties and TRPV1-mediated neuropeptide secretion

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12 December 2020

Evidence that TRPM8 is an androgen-dependent Ca2+ channel required for the survival of prostate cancer cells

1 reference

12 December 2020

The capsaicin-sensitive afferent neuron in skeletal muscle is abnormal in heart failure

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12 December 2020

Effects of inhaled capsaicin in heart-lung transplant patients and asthmatic subjects

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12 December 2020

Human brain endothelium: coexpression and function of vanilloid and endocannabinoid receptors

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12 December 2020

TRPV1 antagonists elevate cell surface populations of receptor protein and exacerbate TRPV1-mediated toxicities in human lung epithelial cells

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12 December 2020

Expression of capsaicin receptor (VR1) by myelinated primary afferent neurons in rats

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12 December 2020

Capsaicin, a double-edged sword: toxicity, metabolism, and chemopreventive potential

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12 December 2020

Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia

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12 December 2020

Evidence for specific TRPM8 expression in human prostate secretory epithelial cells: functional androgen receptor requirement.

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12 December 2020

Co-activation of P2Y2 receptor and TRPV channel by ATP: implications for ATP induced pain

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12 December 2020

The effects of toluene diisocyanate and of capsaicin on human bronchial smooth muscle in vitro

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12 December 2020

Cool (TRPM8) and hot (TRPV1) receptors in the bladder and male genital tract

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12 December 2020

Vanilloid (capsaicin) receptors in health and disease

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12 December 2020

Increased sensitivity of desensitized TRPV1 by PMA occurs through PKCepsilon-mediated phosphorylation at S800.

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12 December 2020

Differential regulation of 3-beta-hydroxysteroid dehydrogenase and vanilloid receptor TRPV1 mRNA in sensory neurons by capsaicin and NGF.

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12 December 2020

TRPV1 activation results in disruption of the blood-brain barrier in the rat

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12 December 2020

Capsaicin receptor TRPV1 in urothelium of neurogenic human bladders and effect of intravesical resiniferatoxin.

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12 December 2020

Regulation of Ca2+-dependent desensitization in the vanilloid receptor TRPV1 by calcineurin and cAMP-dependent protein kinase.

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12 December 2020

Regulation of calcitonin gene-related peptide and TRPV1 in a rat model of osteoarthritis

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12 December 2020

Neurogenic inflammation in human airways: is it important?

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12 December 2020

Expression of the transient receptor potential vanilloid 1 (TRPV1) in LNCaP and PC-3 prostate cancer cells and in human prostate tissue.

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12 December 2020

Vanilloid receptor 1 expression in human tooth pulp in relation to caries and pain

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12 December 2020

TRP channels in airway smooth muscle as therapeutic targets

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12 December 2020

Gastroprotection induced by capsaicin in healthy human subjects.

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12 December 2020

Distinct thymocyte subsets express the vanilloid receptor VR1 that mediates capsaicin-induced apoptotic cell death

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12 December 2020

Nerve growth factor and vanilloid receptor expression, and detrusor instability, after relieving bladder outlet obstruction in rats.

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12 December 2020

The mechanosensitivity of mouse colon afferent fibers and their sensitization by inflammatory mediators require transient receptor potential vanilloid 1 and acid-sensing ion channel 3.

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12 December 2020

An alternative splicing product of the murine trpv1 gene dominant negatively modulates the activity of TRPV1 channels

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12 December 2020

Genetic influence on variability in human acute experimental pain sensitivity associated with gender, ethnicity and psychological temperament

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12 December 2020

Atopy in cough sensitivity to capsaicin and bronchial responsiveness in young females

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12 December 2020

TRP channels as new pharmacological targets

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12 December 2020

An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors

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12 December 2020

Activation and activators of TRPV1 and their pharmaceutical implication

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12 December 2020

TRPV1 gene knockout impairs postischemic recovery in isolated perfused heart in mice

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12 December 2020

cAMP-dependent protein kinase regulates desensitization of the capsaicin receptor (VR1) by direct phosphorylation

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12 December 2020

p38 MAPK activation by NGF in primary sensory neurons after inflammation increases TRPV1 levels and maintains heat hyperalgesia

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12 December 2020

Capsaicin responsiveness and cough in asthma and chronic obstructive pulmonary disease

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12 December 2020

Clinical applications of capsaicinoids

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12 December 2020

Dose-dependent effects of capsaicin nasal challenge: in vivo evidence of human airway neurogenic inflammation

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12 December 2020

TRPV1 receptor: a target for the treatment of pain, cough, airway disease and urinary incontinence

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12 December 2020

Protein kinase C(alpha) is required for vanilloid receptor 1 activation. Evidence for multiple signaling pathways

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12 December 2020

Transient receptor potential vanilloid subfamily 1 expressed in pancreatic islet beta cells modulates insulin secretion in rats

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12 December 2020

Noxious cold ion channel TRPA1 is activated by pungent compounds and bradykinin

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12 December 2020

Analysis of the native quaternary structure of vanilloid receptor 1.

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12 December 2020

Vanilloid and TRP channels: a family of lipid-gated cation channels.

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12 December 2020

Vanilloid receptor (TRPV1)-deficient mice show increased susceptibility to dinitrobenzene sulfonic acid induced colitis

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12 December 2020

Expression of vanilloid receptor subtype 1 in cutaneous sensory nerve fibers, mast cells, and epithelial cells of appendage structures.

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12 December 2020

Diabetic neuropathy: an intensive review

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12 December 2020

Jejunal afferent nerve sensitivity in wild-type and TRPV1 knockout mice

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12 December 2020

Regulated exocytosis contributes to protein kinase C potentiation of vanilloid receptor activity

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12 December 2020

Immunological role of neuronal receptor vanilloid receptor 1 expressed on dendritic cells

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12 December 2020

A TRP channel that senses cold stimuli and menthol

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12 December 2020

Increased anandamide induced relaxation in mesenteric arteries of cirrhotic rats: role of cannabinoid and vanilloid receptors

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12 December 2020

Neurotrophin-3 suppresses thermal hyperalgesia associated with neuropathic pain and attenuates transient receptor potential vanilloid receptor-1 expression in adult sensory neurons.

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12 December 2020

Identification of a tetramerization domain in the C terminus of the vanilloid receptor.

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12 December 2020

Anandamide and arachidonic acid use epoxyeicosatrienoic acids to activate TRPV4 channels

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12 December 2020

Somatostatin modulates the transient receptor potential vanilloid 1 (TRPV1) ion channel

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12 December 2020

Mechanism underlying inhibition of the capsaicin receptor-mediated current by pregnenolone sulfate in rat dorsal root ganglion neurons

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12 December 2020

Investigation of the role of TRPV1 receptors in acute and chronic nociceptive processes using gene-deficient mice

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12 December 2020

Impaired nociception and pain sensation in mice lacking the capsaicin receptor

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12 December 2020

Conservation of functional and pharmacological properties in the distantly related temperature sensors TRVP1 and TRPM8.

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12 December 2020

Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI rats

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12 December 2020

Activity and expression of the vanilloid receptor 1 (TRPV1) is altered by long-term diabetes in epineurial arterioles of the rat sciatic nerve

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12 December 2020

Direct phosphorylation of capsaicin receptor VR1 by protein kinase Cepsilon and identification of two target serine residues

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12 December 2020

Biochemical pharmacology of the vanilloid receptor TRPV1. An update

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12 December 2020

Sex differences in pain perception and anxiety. A psychophysical study with topical capsaicin.

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12 December 2020

Glial cell line derived neurotrophic factor (GDNF) regulates VR1 and substance P in cultured sensory neurons

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12 December 2020

Extensive co-localization and heteromultimer formation of the vanilloid receptor-like protein TRPV2 and the capsaicin receptor TRPV1 in the adult rat cerebral cortex

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12 December 2020

Distribution of mRNA for vanilloid receptor subtype 1 (VR1), and VR1-like immunoreactivity, in the central nervous system of the rat and human

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12 December 2020

Contribution of vanilloid receptors to the overt nociception induced by B2 kinin receptor activation in mice.

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12 December 2020

Induction of vanilloid receptor channel activity by protein kinase C

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12 December 2020

Increased expression of transient receptor potential vanilloid-1 in airway nerves of chronic cough

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12 December 2020

Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia

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12 December 2020

Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances

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12 December 2020

Recent developments in transient receptor potential vanilloid receptor 1 agonist-based therapies

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12 December 2020

NGF rapidly increases membrane expression of TRPV1 heat-gated ion channels.

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12 December 2020

Changes in levels of nerve growth factor in nasal secretions after capsaicin inhalation in patients with airway symptoms from scents and chemicals

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12 December 2020

The epithelial calcium channels TRPV5 and TRPV6: regulation and implications for disease

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12 December 2020

Essential role of Rac1/NADPH oxidase in nerve growth factor induction of TRPV1 expression

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12 December 2020

Capsaicinoids Cause Inflammation and Epithelial Cell Death through Activation of Vanilloid Receptors

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12 December 2020

The distribution of sensory fibers immunoreactive for the TRPV1 (capsaicin) receptor in the human prostate

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12 December 2020

Vanilloid receptor 1 antagonists attenuate disease severity in dextran sulphate sodium-induced colitis in mice

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12 December 2020

Vanilloid receptor expression suggests a sensory role for urinary bladder epithelial cells.

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12 December 2020

Signalling pathways involved in the sensitisation of mouse nociceptive neurones by nerve growth factor

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12 December 2020

Sensitization of vanilloid receptor involves an increase in the phosphorylated form of the channel

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12 December 2020

Endovanilloid signaling in pain

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12 December 2020

Vanilloid (Capsaicin) receptors and mechanisms

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12 December 2020

Compounds acting at the endocannabinoid and/or endovanilloid systems reduce hyperkinesia in a rat model of Huntington's disease

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12 December 2020

Effects of peripheral nerve injury on functional spinal VR1 receptors

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12 December 2020

Vanilloid receptor activation by 2- and 10-μm particles induces responses leading to apoptosis in human airway epithelial cells

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12 December 2020

Reduced thermal sensitivity and Nav1.8 and TRPV1 channel expression in sensory neurons of aged mice

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12 December 2020

Transient receptor potential ion channels as targets for the discovery of pain therapeutics.

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12 December 2020

Competitive inhibition of the capsaicin receptor-mediated current by dehydroepiandrosterone in rat dorsal root ganglion neurons

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12 December 2020

Transient receptor potential vanilloid type 1 (TRPV1) expression changes from normal urothelium to transitional cell carcinoma of human bladder

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12 December 2020

New perspectives on enigmatic vanilloid receptors.

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12 December 2020

Attenuation of thermal nociception and hyperalgesia by VR1 blockers

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12 December 2020

Increased capsaicin receptor TRPV1 nerve fibres in the inflamed human oesophagus.

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12 December 2020

Involvement of transient receptor potential vanilloid 1 in the vascular and hyperalgesic components of joint inflammation.

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12 December 2020

Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain.

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12 December 2020

Impaired thermosensation in mice lacking TRPV3, a heat and camphor sensor in the skin.

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12 December 2020

Sensory fibres expressing capsaicin receptor TRPV1 in patients with rectal hypersensitivity and faecal urgency

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12 December 2020

Vanilloid receptor 1 immunoreactivity in inflamed human bowel

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12 December 2020

Homo- and heteromeric assembly of TRPV channel subunits.

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12 December 2020

PI(4,5)P2 regulates the activation and desensitization of TRPM8 channels through the TRP domain

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12 December 2020

Increased Expression of Vanilloid Receptor 1 on Myelinated Primary Afferent Neurons Contributes to the Antihyperalgesic Effect of Capsaicin Cream in Diabetic Neuropathic Pain in Mice

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12 December 2020

Decreased sensory receptors P2X3 and TRPV1 in suburothelial nerve fibers following intradetrusor injections of botulinum toxin for human detrusor overactivity.

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12 December 2020

Differential expression of the mRNA for the vanilloid receptor subtype 1 in cells of the adult rat dorsal root and nodose ganglia and its downregulation by axotomy

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12 December 2020

Protein kinase C contributes to abnormal capsaicin responses in DRG neurons from cats with feline interstitial cystitis

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12 December 2020

Increased vanilloid receptor VR1 innervation in vulvodynia

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12 December 2020

Relaxant effect of capsazepine in the isolated rat ileum

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12 December 2020

Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide

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12 December 2020

The capsaicin receptor: a heat-activated ion channel in the pain pathway

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12 December 2020

Resiniferatoxin: an ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons

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12 December 2020

Activation of epidermal vanilloid receptor-1 induces release of proinflammatory mediators in human keratinocytes.

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12 December 2020

Vanilloid receptor loss in rat sensory ganglia associated with long term desensitization to resiniferatoxin

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12 December 2020

Diversity of TRP channel activation.

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12 December 2020

Bradykinin and nerve growth factor release the capsaicin receptor from PtdIns(4,5)P2-mediated inhibition

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12 December 2020

Phosphorylation of vanilloid receptor 1 by Ca2+/calmodulin-dependent kinase II regulates its vanilloid binding

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12 December 2020

Direct interaction of adenosine with the TRPV1 channel protein.

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12 December 2020

Evidence for a novel protective role of the vanilloid TRPV1 receptor in a cutaneous contact allergic dermatitis model.

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12 December 2020

Sex-linked differences in the vasorelaxant effects of anandamide in vascular mesenteric beds: role of oestrogens

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12 December 2020

Medium and large injured dorsal root ganglion cells increase TRPV-1, accompanied by increased alpha2C-adrenoceptor co-expression and functional inhibition by clonidine

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12 December 2020

N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neu

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12 December 2020

TRPV1 desensitisation and endogenous vanilloid involvement in the enhanced analgesia induced by capsaicin in inflamed tissues

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12 December 2020

Identification and characterization of a Ca2+ -sensitive interaction of the vanilloid receptor TRPV1 with tubulin

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12 December 2020

TRPV1 (vanilloid receptor) in the urinary tract: expression, function and clinical applications.

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12 December 2020

The cAMP-dependent kinase pathway does not sensitize the cloned vanilloid receptor type 1 expressed in xenopus oocytes or Aplysia neurons.

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12 December 2020

Increased capsaicin receptor TRPV1 in skin nerve fibres and related vanilloid receptors TRPV3 and TRPV4 in keratinocytes in human breast pain

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12 December 2020

Inflammatory mediators convert anandamide into a potent activator of the vanilloid type 1 transient receptor potential receptor in nociceptive primary sensory neurons

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12 December 2020

10.1007/S00210-006-0072-3

Identifiers

DOI

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14 August 2017

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