INT64201

Context Info Confidence 0.59 First Reported 1996 Last Reported 2010 Negated 3 Speculated 8 Reported most in Abstract Documents 203 Total Number 213 Disease Relevance 79.18 Pain Relevance 119.75

cytosol (Trpv1) plasma membrane (Trpv1) lipid metabolic process (Trpv1)

Anatomy Link Frequency neurons 16 DRG 11 spinal cord 5 plasma 5 nociceptor 4 Trpv1 (Rattus norvegicus)

Pain Link Frequency Relevance Heat qutenza 3293 100.00 Pain 1132 100.00 Inflammation 996 100.00 antagonist 747 100.00 dorsal root ganglion 677 100.00 agonist 654 100.00 TRP channel 481 100.00 Calcitonin gene-related peptide 366 100.00 Spinal cord 350 100.00 nociceptor 234 100.00

Disease Link Frequency Relevance Heat Ganglion Cysts 1166 100.00 Pain 1141 100.00 INFLAMMATION 893 100.00 Neuropathic Pain 543 100.00 Nociception 487 100.00 Hyperalgesia 463 99.96 Targeted Disruption 36 99.96 Spinal Cord Injury 82 99.92 Injury 135 99.88 Fever 128 99.78

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

These results extend our previous findings demonstrating that the neonatal treatment of rats with polygodial or drimanial, similar to that reported for capsaicin, produced persistent antinociception in adult animals associated with TRPV1 down-regulation in the spinal cord, but not TRPV1 expression in DRG.

Negative_regulation (down-regulation) of TRPV1 in DRG associated with antinociception, qutenza and spinal cord

1) Confidence 0.59 Published 2004 Journal Neuropharmacology Section Abstract Doc Link 14975683 Disease Relevance 0.20 Pain Relevance 0.99

In vitro, BCTC inhibited capsaicin (300 nM)-induced releases of calcitonin gene-related peptide-like immunoreactivity (CGRP-LI) and substance P-like immunoreactivity (SP-LI) from the rat spinal cord slice preparations with IC(50)s of 37.0 and 36.0 nM, respectively, confirming that BCTC potently inhibits TRPV1 function in the rat spinal cord.

Negative_regulation (inhibits) of TRPV1 in spinal cord associated with qutenza, spinal cord, substance p and calcitonin gene-related peptide

2) Confidence 0.59 Published 2005 Journal Neuropharmacology Section Abstract Doc Link 15998524 Disease Relevance 0.92 Pain Relevance 1.25

Capsaicin-induced desensitization of VR1 was down-regulated, whereas VR1 re-sensitization was up-regulated in DRG neurons from diabetic rats.

Negative_regulation (desensitization) of VR1 in neurons associated with dorsal root ganglion, qutenza and diabetes mellitus

3) Confidence 0.59 Published 2005 Journal J. Biol. Chem. Section Abstract Doc Link 15513920 Disease Relevance 1.68 Pain Relevance 1.22

Compared with the controls, VR1 protein was decreased in DRG whole-cell homogenates from diabetic rats, but increased levels of VR1 protein were observed on plasma membranes.

Negative_regulation (decreased) of VR1 in DRG associated with dorsal root ganglion and diabetes mellitus

4) Confidence 0.59 Published 2005 Journal J. Biol. Chem. Section Abstract Doc Link 15513920 Disease Relevance 1.85 Pain Relevance 1.29

A reduction of TRPV1 protein in membrane fractions was found following cholesterol depletion.

Negative_regulation (reduction) of TRPV1

5) Confidence 0.59 Published 2006 Journal Eur. J. Neurosci. Section Abstract Doc Link 16800863 Disease Relevance 0.08 Pain Relevance 0.44

Inhibition of TRPV1 channels by AG489 is strongly voltage-dependent, with relief of inhibition at positive voltages, consistent with the toxin inhibiting the channel through a pore-blocking mechanism.

Negative_regulation (Inhibition) of TRPV1 in pore

6) Confidence 0.59 Published 2005 Journal Biochemistry Section Abstract Doc Link 16300403 Disease Relevance 0 Pain Relevance 0.07

The mechanism via which ruthenium red selectively inhibited vagal afferent fibres during ischaemia is unknown, but it does not appear to involve blockade of the TRPV1 receptor.

Negative_regulation (blockade) of TRPV1 receptor associated with cv unclassified under development

7) Confidence 0.59 Published 2005 Journal Neurogastroenterol. Motil. Section Abstract Doc Link 15670270 Disease Relevance 0.76 Pain Relevance 0.09

In this paper we investigated the effect of blockade of vanilloid receptor 1 (Transient Receptor Potential Vanilloid Receptor 1 [TRPV1]) on concentrated ambient particles (CAPs)-induced cardiac oxidative stress and dysfunction in a rat model of inhalation exposure.

Spec (investigated) Negative_regulation (blockade) of vanilloid receptor 1 associated with stress

8) Confidence 0.59 Published 2008 Journal Toxicol. Sci. Section Abstract Doc Link 18184637 Disease Relevance 0.32 Pain Relevance 0.04

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

Negative_regulation (blockade) of TRPV1 associated with qutenza, antagonist and fever

9) Confidence 0.59 Published 2007 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 17652633 Disease Relevance 0.38 Pain Relevance 1.07

These findings suggest that nefopam exerts its analgesic and antihyperalgesic effects through multiple mechanisms including blockade of TRPV1 in addition to voltage-dependent calcium channels in the DRG.

Negative_regulation (blockade) of TRPV1 in DRG associated with dorsal root ganglion, antihyperalgesic, calcium channel and analgesic

10) Confidence 0.58 Published 2009 Journal Pharmacology Section Abstract Doc Link 19096234 Disease Relevance 0.25 Pain Relevance 0.84

The camphor-induced desensitization of TRPV1 and block of TRPA1 may underlie the analgesic effects of camphor.

Negative_regulation (desensitization) of TRPV1 associated with analgesic

11) Confidence 0.58 Published 2005 Journal J. Neurosci. Section Abstract Doc Link 16192383 Disease Relevance 0 Pain Relevance 0.81

Using such a combination strategy to produce analgesia may potentially provide an improved therapeutic separation from unwanted in vivo side effects associated with blockade of either Nav1.8 or TRPV1 alone.

Negative_regulation (blockade) of TRPV1 associated with nav1.8 and analgesia

12) Confidence 0.58 Published 2009 Journal J Pain Section Abstract Doc Link 19070548 Disease Relevance 0.60 Pain Relevance 1.25

Axotomy results in the downregulation of VR1 mRNA in dorsal root ganglion cells.

Negative_regulation (downregulation) of VR1 mRNA in dorsal root ganglion associated with ganglion cysts, dorsal root ganglion and vanilloid receptor subtype 1

13) Confidence 0.58 Published 1999 Journal J. Neurosci. Section Abstract Doc Link 10024368 Disease Relevance 0.33 Pain Relevance 1.14

Both TRPV1 and TRPM8 currents were reduced but not eliminated by 4 hr incubation in saturating agonist concentration.

Neg (not) Negative_regulation (reduced) of TRPV1 associated with agonist

14) Confidence 0.58 Published 2009 Journal PLoS ONE Section Abstract Doc Link PMC2780724 Disease Relevance 0.16 Pain Relevance 0.18

Inhibition of the vanilloid receptor subtype-1 attenuates TNBS-colitis.

Negative_regulation (Inhibition) of vanilloid receptor subtype-1 associated with colitis and qutenza

15) Confidence 0.58 Published 2004 Journal J. Gastrointest. Surg. Section Title Doc Link 15531237 Disease Relevance 0.89 Pain Relevance 0.59

Previous reports have indicated that inhibition of VR-1 with capsazepine (CPZ), a VR-1 antagonist, attenuates dextran sodium sulfate (DSS) colitis in rats.

Negative_regulation (inhibition) of VR-1 associated with colitis and antagonist

16) Confidence 0.58 Published 2004 Journal J. Gastrointest. Surg. Section Abstract Doc Link 15531237 Disease Relevance 0.73 Pain Relevance 0.17

Consistent with the loss of TRPV1 expressing central nerve terminals, the immunoreactivity of CGRP and SP associated with TRPV1 immunoreactivity was also significantly reduced (p<0.001) (Fig. 6E, F).

Negative_regulation (loss) of TRPV1 in nerve

17) Confidence 0.58 Published 2009 Journal PLoS ONE Section Body Doc Link PMC2737142 Disease Relevance 0.56 Pain Relevance 0.57

Cross-inhibition between native and recombinant TRPV1 and P2X(3) receptors.

Negative_regulation (inhibition) of TRPV1

18) Confidence 0.57 Published 2009 Journal Pain Section Title Doc Link 19223122 Disease Relevance 0.53 Pain Relevance 0.47

Therefore, these data show that: (1) HS upregulates mesenteric VR1 expression; (2) HS increases sensitivity of blood pressure to AEA; and (3) HS-induced enhancement of the depressor effect of AEA can be prevented only when both VR1 and CB1 receptors are blocked.

Negative_regulation (blocked) of VR1 in blood

19) Confidence 0.57 Published 2005 Journal Hypertension Section Abstract Doc Link 16144988 Disease Relevance 0 Pain Relevance 0.29

This was accompanied by a decrease in spinal cord TRPV1 and CGRP, but not in IB4 binding sensory fibres.

Negative_regulation (decrease) of TRPV1 in spinal cord associated with spinal cord

20) Confidence 0.57 Published 2008 Journal Exp. Neurol. Section Abstract Doc Link 18824169 Disease Relevance 0.93 Pain Relevance 0.68

General Comments

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