The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept (Q36803753)

16 August 2017

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title

The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept (English)

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16 August 2017

Arpad Szallasi

1

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16 August 2017

Daniel N Cortright

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2

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16 August 2017

Charles A Blum

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3

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16 August 2017

Samer R Eid

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4

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16 August 2017

1 May 2007

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Nature Reviews Drug Discovery

16 August 2017

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16 August 2017

6

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16 August 2017

5

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16 August 2017

357-372

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https://scigraph.springernature.com/pub.10.1038/nrd2280

16 August 2017

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Local effector functions of capsaicin-sensitive sensory nerve endings: involvement of tachykinins, calcitonin gene-related peptide and other neuropeptides

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Novel expression of vanilloid receptor 1 on capsaicin-insensitive fibers accounts for the analgesic effect of capsaicin cream in neuropathic pain.

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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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New perspectives on enigmatic vanilloid receptors.

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Vanilloid (capsaicin) receptors in health and disease

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Impaired nociception and pain sensation in mice lacking the capsaicin receptor

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Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia

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ThermoTRP channels and cold sensing: what are they really up to?

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Trp ion channels and temperature sensation

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Nociception and TRP Channels

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Functional aspects and mechanisms of TRPV1 involvement in neurogenic inflammation that leads to thermal hyperalgesia

31 March 2020

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The cloned capsaicin receptor integrates multiple pain-producing stimuli

31 March 2020

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Acid potentiation of the capsaicin receptor determined by a key extracellular site

31 March 2020

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Specific Involvement of PKC-ε in Sensitization of the Neuronal Response to Painful Heat

31 March 2020

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

31 March 2020

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Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide

31 March 2020

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

31 March 2020

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

31 March 2020

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Bradykinin-12-lipoxygenase-VR1 signaling pathway for inflammatory hyperalgesia.

31 March 2020

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Sensitization of TRPV1 by EP1 and IP reveals peripheral nociceptive mechanism of prostaglandins

31 March 2020

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Potentiation of capsaicin receptor activity by metabotropic ATP receptors as a possible mechanism for ATP-evoked pain and hyperalgesia

31 March 2020

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Impaired nociception and inflammatory pain sensation in mice lacking the prokineticin receptor PKR1: focus on interaction between PKR1 and the capsaicin receptor TRPV1 in pain behavior.

31 March 2020

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Polyamines are potent ligands for the capsaicin receptor TRPV1.

31 March 2020

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Jellyfish and other cnidarian envenomations cause pain by affecting TRPV1 channels

31 March 2020

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Spider toxins activate the capsaicin receptor to produce inflammatory pain.

31 March 2020

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

31 March 2020

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Induction of vanilloid receptor channel activity by protein kinase C

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin

31 March 2020

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The mu opioid agonist morphine modulates potentiation of capsaicin-evoked TRPV1 responses through a cyclic AMP-dependent protein kinase A pathway

31 March 2020

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Co-expression of the voltage-gated potassium channel Kv1.4 with transient receptor potential channels (TRPV1 and TRPV2) and the cannabinoid receptor CB1 in rat dorsal root ganglion neurons

31 March 2020

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Delta (delta) opioid receptors in small and medium-sized trigeminal neurons supporting the dental pulp of rats

31 March 2020

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

31 March 2020

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High-affinity partial agonists of the vanilloid receptor

31 March 2020

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Molecular basis for species-specific sensitivity to "hot" chili peppers

31 March 2020

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Functional mapping of the transient receptor potential vanilloid 1 intracellular binding site.

31 March 2020

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Functional characterisation of the S512Y mutant vanilloid human TRPV1 receptor

31 March 2020

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Gadolinium activates and sensitizes the vanilloid receptor TRPV1 through the external protonation sites

31 March 2020

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A polyclonal antibody to the prepore loop of transient receptor potential vanilloid type 1 blocks channel activation.

31 March 2020

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A hot-sensing cold receptor: C-terminal domain determines thermosensation in transient receptor potential channels.

31 March 2020

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Forty years in capsaicin research for sensory pharmacology and physiology

31 March 2020

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Cloning of a stretch-inhibitable nonselective cation channel.

31 March 2020

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The genomic organization of the gene encoding the vanilloid receptor: evidence for multiple splice variants

31 March 2020

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The distribution and regulation of vanilloid receptor VR1 and VR1 5' splice variant RNA expression in rat.

31 March 2020

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Molecular cloning of an N-terminal splice variant of the capsaicin receptor. Loss of N-terminal domain suggests functional divergence among capsaicin receptor subtypes

31 March 2020

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Regulation of TRPV1 by a novel renally expressed rat TRPV1 splice variant

31 March 2020

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

31 March 2020

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TRPV1b, a functional human vanilloid receptor splice variant

31 March 2020

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An N-terminal variant of Trpv1 channel is required for osmosensory transduction

31 March 2020

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A capsaicin-receptor homologue with a high threshold for noxious heat

31 March 2020

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TRPV3 is a temperature-sensitive vanilloid receptor-like protein.

31 March 2020

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Heat-evoked activation of the ion channel, TRPV4.

31 March 2020

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Identification of a cold receptor reveals a general role for TRP channels in thermosensation

31 March 2020

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A TRP channel that senses cold stimuli and menthol

31 March 2020

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ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures

31 March 2020

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Immunocyte Ca2+ influx system mediated by LTRPC2.

31 March 2020

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Regulation of melastatin, a TRP-related protein, through interaction with a cytoplasmic isoform

31 March 2020

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Heat activation of TRPM5 underlies thermal sensitivity of sweet taste

31 March 2020

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Regulation of TRPV5 and TRPV6 by associated proteins

31 March 2020

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

31 March 2020

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

31 March 2020

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Vanilloid receptor 1 immunoreactivity in inflamed human bowel

31 March 2020

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

31 March 2020

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Increased vanilloid receptor VR1 innervation in vulvodynia

31 March 2020

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

31 March 2020

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Expression of capsaicin receptor immunoreactivity in human peripheral nervous system and in painful neuropathies

31 March 2020

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

31 March 2020

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VR1 protein expression increases in undamaged DRG neurons after partial nerve injury

31 March 2020

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Protective role of vanilloid receptor type 1 in HCl-induced gastric mucosal lesions in rats.

31 March 2020

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

31 March 2020

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Vanilloid receptor TRPV1: hot on the tongue and inflaming the colon

31 March 2020

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

31 March 2020

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Hot receptors in the brain

31 March 2020

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TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists

31 March 2020

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The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans

31 March 2020

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Altered urinary bladder function in mice lacking the vanilloid receptor TRPV1

31 March 2020

1 reference

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist

31 March 2020

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Attenuated fever response in mice lacking TRPV1

31 March 2020

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Capsaicin-induced vasoconstriction in the mouse knee joint: a study using TRPV1 knockout mice

31 March 2020

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Attenuation of experimental arthritis in TRPV1R knockout mice.

31 March 2020

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

31 March 2020

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Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture

31 March 2020

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

31 March 2020

1 reference

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.

31 March 2020

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

31 March 2020

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Transient receptor potential vanilloid 1, calcitonin gene-related peptide, and substance P mediate nociception in acute pancreatitis.

31 March 2020

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Transient receptor potential vanilloid (TRPV-1) promotes neurogenic inflammation in the pancreas via activation of the neurokinin-1 receptor (NK-1R).

31 March 2020

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Mouse colon sensory neurons detect extracellular acidosis via TRPV1

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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Anandamide-evoked activation of vanilloid receptor 1 contributes to the development of bladder hyperreflexia and nociceptive transmission to spinal dorsal horn neurons in cystitis.

31 March 2020

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The TRPV1 receptor: target of toxicants and therapeutics

31 March 2020

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The transient receptor potential vanilloid 1: role in airway inflammation and disease

31 March 2020

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Proteinase-activated receptor 2-mediated potentiation of transient receptor potential vanilloid subfamily 1 activity reveals a mechanism for proteinase-induced inflammatory pain.

31 March 2020

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Protease-activated receptor 2 sensitizes TRPV1 by protein kinase Cepsilon- and A-dependent mechanisms in rats and mice

31 March 2020

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Protease-activated receptor-2 activation exaggerates TRPV1-mediated cough in guinea pigs.

31 March 2020

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Capsaicin inhalation in man and the effects of sodium cromoglycate

31 March 2020

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

31 March 2020

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A role for TRPV1 in bradykinin-induced excitation of vagal airway afferent nerve terminals

31 March 2020

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Capsazepine inhibits cough induced by capsaicin and citric acid but not by hypertonic saline in guinea pigs

31 March 2020

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Antitussive activity of iodo-resiniferatoxin in guinea pigs

31 March 2020

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TRPV1 antagonists attenuate antigen-provoked cough in ovalbumin sensitized guinea pigs

31 March 2020

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31 March 2020

Measurement of cough.

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Animal models of cough: literature review and presentation of a novel cigarette smoke-enhanced cough model in the guinea-pig

31 March 2020

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Cough. 7: Current and future drugs for the treatment of chronic cough

31 March 2020

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Calcitonin gene-related peptide antagonists as treatments of migraine and other primary headaches

31 March 2020

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Capsaicin-sensitive neurogenic sensory vasodilatation in the dura mater of the rat.

31 March 2020

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CGRP and migraine: neurogenic inflammation revisited

31 March 2020

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Anandamide acts as a vasodilator of dural blood vessels in vivo by activating TRPV1 receptors

31 March 2020

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Plethysmographic evaluation of the vascular effects of human calcitonin gene-related peptide in man

31 March 2020

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Pathophysiology and therapeutic possibilities of calcitonin gene-related peptide in hypertension

31 March 2020

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A novel mechanism contributing to development of Dahl salt-sensitive hypertension: role of the transient receptor potential vanilloid type 1.

31 March 2020

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Haemodynamic profile and responsiveness to anandamide of TRPV1 receptor knock-out mice

31 March 2020

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Impaired osmotic sensation in mice lacking TRPV4

31 March 2020

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Calcitonin gene-related peptide in myocardial ischaemia and reperfusion in the pig

31 March 2020

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Effect of calcitonin gene-related peptide on coronary microvessels and its role in acute myocardial ischemia

31 March 2020

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The role of calcitonin gene-related peptide (CGRP) in ischemic preconditioning in isolated rat hearts

31 March 2020

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

31 March 2020

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Sensing tissue ischemia: another new function for capsaicin receptors?

31 March 2020

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Cardiac vanilloid receptor 1-expressing afferent nerves and their role in the cardiogenic sympathetic reflex in rats

31 March 2020

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Mitochondrial Changes in Preoptic Neurones after Capsaicin Desensitization of the Hypothalamic Thermodetectors in Rats

31 March 2020

1 reference

Lipopolysaccharide fever is initiated via a capsaicin-sensitive mechanism independent of the subtype-1 vanilloid receptor

31 March 2020

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Presynaptic Facilitation of Glutamatergic Synapses to Dopaminergic Neurons of the Rat Substantia Nigra by Endogenous Stimulation of Vanilloid Receptors

31 March 2020

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Transient receptor potential vanilloid subtype 1 mediates cell death of mesencephalic dopaminergic neurons in vivo and in vitro.

31 March 2020

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Reduced anxiety, conditioned fear, and hippocampal long-term potentiation in transient receptor potential vanilloid type 1 receptor-deficient mice.

31 March 2020

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Autonomic regulation of islet hormone secretion--implications for health and disease

31 March 2020

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

31 March 2020

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Calcitonin gene-related peptide: occurrence in pancreatic islets in the mouse and the rat and inhibition of insulin secretion in the mouse

31 March 2020

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Involvement of capsaicin-sensitive nerves in the regulation of glucose tolerance in diabetic rats

31 March 2020

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Sensory nerve inactivation by resiniferatoxin improves insulin sensitivity in male obese Zucker rats

31 March 2020

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TRPV1+ sensory neurons control beta cell stress and islet inflammation in autoimmune diabetes

31 March 2020

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TRPV1: a therapeutic target for novel analgesic drugs?

31 March 2020

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The TRPV1 receptor and nociception

31 March 2020

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Peripheral inflammation induces up-regulation of TRPV2 expression in rat DRG.

31 March 2020

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A heat-sensitive TRP channel expressed in keratinocytes

31 March 2020

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TRPV3 is a calcium-permeable temperature-sensitive cation channel.

31 March 2020

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2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3.

31 March 2020

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Potentiation of TRPV3 channel function by unsaturated fatty acids

31 March 2020

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

31 March 2020

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Heat-evoked activation of TRPV4 channels in a HEK293 cell expression system and in native mouse aorta endothelial cells

31 March 2020

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Cell swelling, heat, and chemical agonists use distinct pathways for the activation of the cation channel TRPV4.

31 March 2020

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Bisandrographolide from Andrographis paniculata activates TRPV4 channels.

31 March 2020

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Abnormal osmotic regulation in trpv4 -/- mice

31 March 2020

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Impaired Pressure Sensation in Mice Lacking TRPV4

31 March 2020

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Warm temperature-sensitive transient receptor potential vanilloid 4 (TRPV4) plays an essential role in thermal hyperalgesia.

31 March 2020

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Altered thermal selection behavior in mice lacking transient receptor potential vanilloid 4

31 March 2020

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A transient receptor potential vanilloid 4-dependent mechanism of hyperalgesia is engaged by concerted action of inflammatory mediators.

31 March 2020

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

31 March 2020

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TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion

31 March 2020

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Coding of sweet, bitter, and umami tastes: different receptor cells sharing similar signaling pathways

31 March 2020

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Distinct expression of TRPM8, TRPA1, and TRPV1 mRNAs in rat primary afferent neurons with adelta/c-fibers and colocalization with trk receptors

31 March 2020

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Two populations of cold-sensitive neurons in rat dorsal root ganglia and their modulation by nerve growth factor

31 March 2020

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

31 March 2020

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TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents

31 March 2020

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Pungent products from garlic activate the sensory ion channel TRPA1

31 March 2020

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Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1

31 March 2020

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The pungency of garlic: activation of TRPA1 and TRPV1 in response to allicin.

31 March 2020

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TRP channel activation by reversible covalent modification

31 March 2020

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TRPA1 contributes to cold, mechanical, and chemical nociception but is not essential for hair-cell transduction

31 March 2020

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Antisense knock down of TRPA1, but not TRPM8, alleviates cold hyperalgesia after spinal nerve ligation in rats

31 March 2020

1 reference

The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin

31 March 2020

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Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist.

31 March 2020

1 reference

AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties

31 March 2020

1 reference

A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid

31 March 2020

1 reference

N-(4-Tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: I. In Vitro Characterization and Pharmacokinetic Properties

31 March 2020

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Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development

31 March 2020

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Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

31 March 2020

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Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1.

31 March 2020

1 reference

inferred from DOI database lookup

7 January 2021

based on heuristic

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

1 reference

inferred from DOI database lookup

7 January 2021

based on heuristic

Identifiers

DOI

10.1038/NRD2280

1 reference

16 August 2017

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