INT49436

Context Info Confidence 0.48 First Reported 1995 Last Reported 2010 Negated 5 Speculated 3 Reported most in Abstract Documents 145 Total Number 148 Disease Relevance 38.35 Pain Relevance 55.08

cytosol (TRPV1) transport (TRPV1) plasma membrane (TRPV1) lipid metabolic process (TRPV1)

Anatomy Link Frequency pore 5 brain 4 external 4 nerve 4 tail 3 TRPV1 (Homo sapiens) TRPV1 - I585V (1)

Pain Link Frequency Relevance Heat qutenza 651 100.00 agonist 269 100.00 antagonist 158 100.00 TRP channel 63 100.00 Cannabinoid receptor 26 100.00 Dismenorea 10 100.00 vanilloid receptor subtype 1 7 100.00 c fibre 27 99.90 Pain 411 99.88 nociceptor 48 99.88

Disease Link Frequency Relevance Heat Tumor Necrosis Factor Receptor-associated Periodic Syndrome 1 99.98 Stomach Disease 3 99.80 Migraine Disorders 1 99.80 INFLAMMATION 265 99.76 Nociception 176 99.76 Arthritis 90 99.76 Pain 338 99.68 Apoptosis 17 99.64 Hyperalgesia 54 99.56 Neuropathic Pain 128 99.54

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Thus, the discovery of new drugs that can bind the VR1 receptor, or antagonise endogenous inflammatory substances that activate this receptor, could lead to new therapies for pain and dysmotility.

VR1 receptor Binding (bind) of associated with pain and inflammation

1) Confidence 0.48 Published 2001 Journal Lancet Section Abstract Doc Link 11343743 Disease Relevance 0.55 Pain Relevance 0.41

OBJECTIVE: Capsaicin, which acts by binding to the vanilloid receptor-1 (VR1), has been shown to give protection against gastric mucosal injury and to enhance healing of gastric ulcers.

vanilloid receptor-1 Binding (binding) of associated with qutenza, injury and peptic ulcer

2) Confidence 0.48 Published 2005 Journal Scand. J. Gastroenterol. Section Abstract Doc Link 16118913 Disease Relevance 0.19 Pain Relevance 0.18

OBJECTIVE: Capsaicin, which acts by binding to the vanilloid receptor-1 (VR1), has been shown to give protection against gastric mucosal injury and to enhance healing of gastric ulcers.

VR1 Binding (binding) of associated with qutenza, injury and peptic ulcer

3) Confidence 0.48 Published 2005 Journal Scand. J. Gastroenterol. Section Abstract Doc Link 16118913 Disease Relevance 0.19 Pain Relevance 0.18

Thus, rabbit polyclonal antibodies against rat and human TRPV1 prepore region seem to partially lock or stabilize the channel in the closed state, whereas rabbit anti-human TRPV1 monoclonal antibodies bind to the prepore region but do not lock or stabilize the channel conformation.

TRPV1 Binding (bind) of

4) Confidence 0.48 Published 2006 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 16844842 Disease Relevance 0.08 Pain Relevance 0.54

After vanilloid binding to VR-1, these neurons remain transiently desensitized; that is, less reactive to natural stimuli.

VR-1 Binding (binding) of in neurons

5) Confidence 0.48 Published 2002 Journal Urology Section Abstract Doc Link 12007523 Disease Relevance 0.41 Pain Relevance 0.30

Iodine-induced reversal of vanilloid activity was also observed in vanillamides more powerful than capsaicin, but a poor correlation was found between agonistic and antagonistic potencies, suggesting that differences exist in the way vanillamides and their 6'-iodo derivatives bind to TRPV1.' '

TRPV1 Binding (bind) of associated with qutenza

6) Confidence 0.48 Published 2005 Journal J. Med. Chem. Section Abstract Doc Link 16000002 Disease Relevance 0 Pain Relevance 0.28

Our observations demonstrate that gender, ethnicity and temperament contribute to individual variation in thermal and cold pain sensitivity by interactions with TRPV1 and OPRD1 single nucleotide polymorphisms.

TRPV1 Binding (interactions) of associated with pain

7) Confidence 0.47 Published 2004 Journal Pain Section Abstract Doc Link 15157710 Disease Relevance 0.38 Pain Relevance 0.60

Although vanilloid receptors are known to exist and function as homomers [15,16], some evidence has been provided for the biochemical association of TRPV3 and TRPV1 suggesting heteromerization [17], thus allowing a greater range of receptor characteristics.

TRPV1 Binding (association) of

8) Confidence 0.47 Published 2007 Journal BMC Neurol Section Body Doc Link PMC1892784 Disease Relevance 0.58 Pain Relevance 0.68

Furthermore, it has been also emerged that, through associations with other molecules, the vanilloid receptor 1 plays an important role in the integration of various stimuli and modulation of cellular excitability.

vanilloid receptor 1 Binding (associations) of

9) Confidence 0.47 Published 2004 Journal Eur. J. Pharmacol. Section Abstract Doc Link 15464045 Disease Relevance 0.15 Pain Relevance 0.12

Furthermore, AEA binds to the transient receptor potential vanilloid type-1 (TRPV1), a capsaicin-sensitive, non-selective cation channel.

TRPV1 Binding (binds) of associated with qutenza

10) Confidence 0.47 Published 2006 Journal Biochimie Section Abstract Doc Link 16949718 Disease Relevance 0.20 Pain Relevance 0.36

In fact, although ethanol was found to bind TRPV1, it does not cause its desensitization [35].

TRPV1 Binding (bind) of

11) Confidence 0.47 Published 2007 Journal BMC Urol Section Body Doc Link PMC1903357 Disease Relevance 0.30 Pain Relevance 0.17

RTX binding to TRPV1 present in urothelial cells may, therefore, have contributed to urgency improvement by disrupting the cross-talk between urothelial cells and suburothelial C-fibers.

TRPV1 Binding (binding) of in urothelial cells associated with c fibre

12) Confidence 0.47 Published 2007 Journal BMC Urol Section Body Doc Link PMC1903357 Disease Relevance 0.13 Pain Relevance 0.41

In C-fibers RTX binding to TRPV1 causes a massive inflow of calcium and other ions into the fiber, generating action potentials and releasing neuropeptides from peripheral nerve endings [25,26], both events contributing to itch or urgency sensations reported by some patients in the present and in previous studies in which RTX instillation was carried out [14,16].

TRPV1 Binding (binding) of in peripheral nerve associated with action potential, c fibre, pruritus and neuropeptide

13) Confidence 0.47 Published 2007 Journal BMC Urol Section Body Doc Link PMC1903357 Disease Relevance 0.18 Pain Relevance 0.29

Its interaction with VR1 was confirmed by GST-pull-down and co-immunoprecipitation.

VR1 Binding (interaction) of

14) Confidence 0.47 Published 2005 Journal Biochem. Biophys. Res. Commun. Section Abstract Doc Link 15883036 Disease Relevance 0.09 Pain Relevance 0.28

Upon interrogation of a mouse brain library, one gene product that interacts with VR1 and is highly homologous to human eferin was found.

VR1 Binding (interacts) of in brain

15) Confidence 0.47 Published 2005 Journal Biochem. Biophys. Res. Commun. Section Abstract Doc Link 15883036 Disease Relevance 0.08 Pain Relevance 0.28

Yeast two-hybrid and pull-down assays showed that self-association of the TRPV1-C is blocked when segment 684Glu-721Arg is deleted.

TRPV1 Binding (association) of

16) Confidence 0.47 Published 2004 Journal J. Neurosci. Section Abstract Doc Link 15190102 Disease Relevance 0 Pain Relevance 0.11

These findings and those of others reported in the literature indicate reciprocal interactions between TRPV1 and ROS play critical roles in the pathological and nociceptive responses active during arthritic inflammation.

TRPV1 Binding (interactions) of

17) Confidence 0.47 Published 2010 Journal Mol Pain Section Body Doc Link 20691059 Disease Relevance 0 Pain Relevance 0

Based upon these observations, a three-dimensional pharmacophore model for the capsaicin-receptor interactions is proposed.

capsaicin-receptor Binding (interactions) of associated with qutenza

18) Confidence 0.47 Published 1995 Journal J. Comput. Aided Mol. Des. Section Abstract Doc Link 7561979 Disease Relevance 0 Pain Relevance 0.77

The aim of this study was to investigate the interaction of a series of novel compounds with leukotriene B(4) receptors (BLT) and vanilloid receptor (TRPV1).

vanilloid receptor Binding (interaction) of

19) Confidence 0.46 Published 2006 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 16207832 Disease Relevance 0.13 Pain Relevance 0.09

Novel compounds that interact with both leukotriene B4 receptors and vanilloid TRPV1 receptors.

TRPV1 Binding (interact) of

20) Confidence 0.46 Published 2006 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 16207832 Disease Relevance 0.15 Pain Relevance 0.14

General Comments

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