INT96511

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Context Info
Confidence 0.59
First Reported 2001
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 35
Total Number 35
Disease Relevance 10.95
Pain Relevance 19.79

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

cytosol (Trpv1) plasma membrane (Trpv1) lipid metabolic process (Trpv1)
Anatomy Link Frequency
visceral 2
plasma 2
neurons 2
nerve 2
DRG 2
Trpv1 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
qutenza 629 100.00 Very High Very High Very High
Action potential 35 100.00 Very High Very High Very High
spinal dorsal horn 32 100.00 Very High Very High Very High
agonist 84 99.96 Very High Very High Very High
dorsal root ganglion 124 99.84 Very High Very High Very High
Nerve growth factor 119 99.80 Very High Very High Very High
nociceptor 36 99.72 Very High Very High Very High
Potency 14 99.60 Very High Very High Very High
antagonist 176 99.50 Very High Very High Very High
Root ganglion neuron 10 99.04 Very High Very High Very High
Disease Link Frequency Relevance Heat
Nociception 84 99.86 Very High Very High Very High
Ganglion Cysts 198 99.84 Very High Very High Very High
Hypothermia 2 99.12 Very High Very High Very High
Injury 58 98.92 Very High Very High Very High
INFLAMMATION 95 98.76 Very High Very High Very High
Pain 187 98.52 Very High Very High Very High
Hypersensitivity 17 98.32 Very High Very High Very High
Nervous System Injury 16 98.20 Very High Very High Very High
Fever 53 95.60 Very High Very High Very High
Neuropathic Pain 103 95.56 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Blockade of TRPV1 activation by selective antagonists is under investigation in an attempt to identify novel agents for pain treatment.
Negative_regulation (Blockade) of Positive_regulation (activation) of TRPV1 associated with pain and antagonist
1) Confidence 0.59 Published 2010 Journal J. Med. Chem. Section Abstract Doc Link 20307063 Disease Relevance 0.15 Pain Relevance 0.51
Similar to capsazepine, this compound inhibits capsaicin-induced activation of rat VR1 with an IC50 value of 35 nM.
Negative_regulation (inhibits) of Positive_regulation (activation) of VR1 associated with qutenza
2) Confidence 0.59 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12721338 Disease Relevance 0.09 Pain Relevance 0.74
Interestingly however, BCTC also potently inhibits acid-induced activation of rat VR1 (IC50 value of 6.0 nM), whereas capsazepine is inactive.
Negative_regulation (inhibits) of Positive_regulation (activation) of VR1
3) Confidence 0.59 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12721338 Disease Relevance 0.08 Pain Relevance 0.78
Focal application of heated solutions demonstrated that the normal threshold (approximately 42 degrees C) of TRPV1 activation was reduced in the presence of capsaicin (1 microM) to approximately 30 degrees C.
Negative_regulation (reduced) of Positive_regulation (activation) of TRPV1 associated with qutenza
4) Confidence 0.59 Published 2008 Journal Inflamm. Res. Section Abstract Doc Link 18777111 Disease Relevance 0.25 Pain Relevance 0.69
We found that profile C modulator, (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)acrylamide (AMG8562), blocks capsaicin activation of TRPV1, does not affect heat activation of TRPV1, potentiates pH 5 activation of TRPV1 in vitro, and does not cause hyperthermia in vivo in rats.
Negative_regulation (blocks) of Positive_regulation (activation) of TRPV1 associated with qutenza and fever
5) Confidence 0.59 Published 2008 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 18420600 Disease Relevance 0.77 Pain Relevance 0.72
Treatment of WA stress rats in situ with WIN 55,212-2 or the TRPV1 antagonist capsazepine prevented the development of visceral hyperalgesia and blocked the upregulation of TRPV1.
Negative_regulation (blocked) of Positive_regulation (upregulation) of TRPV1 in visceral
6) Confidence 0.58 Published 2009 Journal Gut Section Body Doc Link 18936104 Disease Relevance 0 Pain Relevance 0
Moreover, A-425619 was 25- to 50-fold more potent than capsazepine in blocking TRPV1 activation.
Negative_regulation (blocking) of Positive_regulation (activation) of TRPV1
7) Confidence 0.58 Published 2005 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15837819 Disease Relevance 0.15 Pain Relevance 0.60
Acting extracellularly, the inhibitors prevent TRPV1 activation, therefore the intracellular calmodulin might be secondary and has little if any effect on [Ca2+]i signal induced by inflammatory pain agonists either exo-, or endogenous.
Negative_regulation (prevent) of Positive_regulation (activation) of TRPV1 associated with ipn and agonist
8) Confidence 0.52 Published 2007 Journal PLoS ONE Section Body Doc Link PMC1890308 Disease Relevance 0.10 Pain Relevance 0.46
Although blockade of capsaicin-induced VR1 activation has been demonstrated in vitro and in vivo with the antagonist capsazepine, efficacy in rat models of chronic pain has not been observed with this compound.
Negative_regulation (blockade) of Positive_regulation (activation) of VR1 associated with qutenza, lasting pain and antagonist
9) Confidence 0.43 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12721338 Disease Relevance 0.10 Pain Relevance 0.66
We hypothesized that if group B antagonists bind at the same or an overlapping binding pocket of TRPV1 as group A antagonists, and proton activation does not alter the binding pocket, then group B antagonists should compete with and prevent group A antagonism of TRPV1 activation by protons.
Negative_regulation (prevent) of Positive_regulation (activation) of TRPV1 associated with antagonist
10) Confidence 0.43 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 16135784 Disease Relevance 0 Pain Relevance 1.17
Taken together, our results indicate that curcumin blocks capsaicin-induced TRPV1 activation and thereby inhibits TRPV1-mediated pain hypersensitivity.
Negative_regulation (blocks) of Positive_regulation (activation) of TRPV1 associated with qutenza, hypersensitivity and stimulus evoked pain
11) Confidence 0.43 Published 2010 Journal J. Dent. Res. Section Abstract Doc Link 20040737 Disease Relevance 0.96 Pain Relevance 0.75
UTP, a P2Y purinoceptor 2 (P2Y(2))/P2Y(4) receptor agonist, reversed capsaicin-induced TRPV1 desensitization. 2-methyl-thio-ATP (2-Me-S-ATP), a P2Y(1) receptor agonist, did not change desensitization.
Negative_regulation (reversed) of Positive_regulation (induced) of TRPV1 associated with qutenza and agonist
12) Confidence 0.43 Published 2010 Journal Am. J. Physiol. Regul. Integr. Comp. Physiol. Section Abstract Doc Link 20335377 Disease Relevance 0 Pain Relevance 0.59
Since many nociceptors express TRPV1, it is possible that local tissue-cooling may inhibit nociceptor activity via reduction of TRPV1 activation.
Negative_regulation (reduction) of Positive_regulation (activation) of TRPV1 in nociceptor associated with nociceptor
13) Confidence 0.43 Published 2006 Journal J. Dent. Res. Section Abstract Doc Link 17062748 Disease Relevance 0 Pain Relevance 0.71
The rat vanilloid receptor splice variant VR.5'sv blocks TRPV1 activation.
Negative_regulation (blocks) of Positive_regulation (activation) of TRPV1
14) Confidence 0.43 Published 2007 Journal Neuroreport Section Title Doc Link 17558279 Disease Relevance 0.16 Pain Relevance 0.28
AMG8562 blocks capsaicin activation of TRPV1 receptor, does not affect heat activation of TRPV1 receptor, potentiates pH 5 activation of TRPV1 receptor in vitro, and does not cause hyperthermia in vivo in rats.
Negative_regulation (blocks) of Positive_regulation (activation) of TRPV1 receptor associated with qutenza and fever
15) Confidence 0.43 Published 2010 Journal Mol Pain Section Body Doc Link PMC2959024 Disease Relevance 0.65 Pain Relevance 0.47
A-425619 showed similar potency (IC50 = 3-4 nM) to block TRPV1 receptor activation by anandamide and N-arachidonoyl-dopamine.
Negative_regulation (block) of Positive_regulation (activation) of TRPV1 associated with dopamine and potency
16) Confidence 0.43 Published 2005 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15837819 Disease Relevance 0.17 Pain Relevance 0.62
Electrophysiological experiments showed that A-425619 also potently blocked the activation of native TRPV1 channels in rat dorsal root ganglion neurons (IC50 = 9 nM).
Negative_regulation (blocked) of Positive_regulation (activation) of TRPV1 in neurons associated with ganglion cysts and root ganglion neuron
17) Confidence 0.43 Published 2005 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15837819 Disease Relevance 0.18 Pain Relevance 0.63
Paratracheal injection of short interfering RNA targeting TRPV1 blocked TRPV1 up-regulation in cervical DRG and abolished inflammation-mediated HPL reductions seen at 50 degrees C.
Negative_regulation (blocked) of Positive_regulation (up-regulation) of TRPV1 in DRG associated with inflammation
18) Confidence 0.43 Published 2007 Journal Eur. J. Neurosci. Section Abstract Doc Link 17509082 Disease Relevance 1.63 Pain Relevance 0.98
Evoked synaptic current recordings show synaptic failures that are likely to be due to depolarization block from sustained TRPV1 activation.
Negative_regulation (block) of Positive_regulation (activation) of TRPV1
19) Confidence 0.42 Published 2009 Journal PLoS ONE Section Body Doc Link PMC2737142 Disease Relevance 0.71 Pain Relevance 0.88
Thus, the inhibition of TRPV1 activation by dexbrompheniramine may provide one potential mechanism whereby this antihistamine exerts its therapeutic effect in chronic cough.
Negative_regulation (inhibition) of Positive_regulation (activation) of TRPV1 associated with antihistamine and cough
20) Confidence 0.42 Published 2008 Journal Exp. Lung Res. Section Abstract Doc Link 19085565 Disease Relevance 0.21 Pain Relevance 0.57

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