Screening TRPV1 antagonists for the treatment of pain: lessons learned over a decade (Q38088356)

28 August 2017

Screening TRPV1 antagonists for the treatment of pain: lessons learned over a decade (English)

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28 August 2017

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József Lázár

1

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28 August 2017

Laxmikant Gharat

2

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28 August 2017

Neelima Khairathkar-Joshi

3

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28 August 2017

Peter M Blumberg

4

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28 August 2017

Arpad Szallasi

5

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28 August 2017

language of work or name

English

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publication date

1 February 2009

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Expert Opinion on Drug Discovery

28 August 2017

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28 August 2017

4

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28 August 2017

2

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28 August 2017

159-180

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Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival?

28 August 2017

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Cloning and functional expression of a human orthologue of rat vanilloid receptor-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Structure of TRPV1 channel revealed by electron cryomicroscopy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

A role of the transient receptor potential domain of vanilloid receptor I in channel gating.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

ThermoTRP channels as modular proteins with allosteric gating.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Molecular determinants of vanilloid sensitivity in TRPV1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Camphor activates and strongly desensitizes the transient receptor potential vanilloid subtype 1 channel in a vanilloid-independent mechanism.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Spider toxins activate the capsaicin receptor to produce inflammatory pain.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Biochemistry and pharmacology of endovanilloids

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Novel gating and sensitizing mechanism of capsaicin receptor (TRPV1): tonic inhibitory regulation of extracellular sodium through the external protonation sites on TRPV1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Immunocytochemical localization of the vanilloid receptor 1 (VR1): relationship to neuropeptides, the P2X3 purinoceptor and IB4 binding sites

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Biochemical pharmacology of the vanilloid receptor TRPV1. An update

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460440802681300

Phosphoinositide 3-kinase binds to TRPV1 and mediates NGF-stimulated TRPV1 trafficking to the plasma membrane.

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460440802681300

Hot channels in airways: pharmacology of the vanilloid receptor.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Protein kinase A anchoring via AKAP150 is essential for TRPV1 modulation by forskolin and prostaglandin E2 in mouse sensory neurons

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Proinflammatory mediators modulate the heat-activated ion channel TRPV1 via the scaffolding protein AKAP79/150

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Association of protein kinase A and protein phosphatase 2B with a common anchoring protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Coordination of three signaling enzymes by AKAP79, a mammalian scaffold protein

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Histamine-induced Ca(2+) influx via the PLA(2)/lipoxygenase/TRPV1 pathway in rat sensory neurons

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Dual regulation of TRPV1 by phosphoinositides.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pirt, a phosphoinositide-binding protein, functions as a regulatory subunit of TRPV1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Induction of vanilloid receptor channel activity by protein kinase C

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Protein kinase C activation potentiates gating of the vanilloid receptor VR1 by capsaicin, protons, heat and anandamide

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Protein kinase C phosphorylation sensitizes but does not activate the capsaicin receptor transient receptor potential vanilloid 1 (TRPV1).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Endogenous tumor necrosis factor alpha (TNFalpha) requires TNF receptor type 2 to generate heat hyperalgesia in a mouse cancer model

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Interaction between protein kinase Cmu and the vanilloid receptor type 1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pharmacological differences between the human and rat vanilloid receptor 1 (VR1)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Cloning and functional characterization of the guinea pig vanilloid receptor 1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pain research update from a genetic point of view.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Are mu-opioid receptor polymorphisms important for clinical opioid therapy?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Genetic predictors for acute experimental cold and heat pain sensitivity in humans

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Genetic mutations that prevent pain: implications for future pain medication

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Functional effects of nonsynonymous polymorphisms in the human TRPV1 gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Cloning and pharmacological characterization of mouse TRPV1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

5-Iodoresiniferatoxin evokes hypothermia in mice and is a partial transient receptor potential vanilloid 1 agonist in vitro

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Kinetics of penetration influence the apparent potency of vanilloids on TRPV1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

High affinity antagonists of the vanilloid receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

The role of transient receptor potential vanilloid 1 in mechanical and chemical visceral hyperalgesia following experimental colitis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Transient receptor potential vanilloid 1 agonists cause endoplasmic reticulum stress and cell death in human lung cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

4-(2-Pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Studies on somnolence in the daytime caused by drugs used for neuropathic pain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Discovery of small molecule antagonists of TRPV1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

(R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Increasingly irritable and close to tears: TRPA1 in inflammatory pain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Mechanism of action of analgesics used to treat osteoarthritis pain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Neurogenic responses mediated by vanilloid receptor-1 (TRPV1) are blocked by the high affinity antagonist, iodo-resiniferatoxin

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460440802681300

10.1517/17460440802681300

21 January 2018

Identifiers

DOI

1 reference

28 August 2017

1 reference