INT77902

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Context Info
Confidence 0.59
First Reported 1998
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 30
Total Number 30
Disease Relevance 9.36
Pain Relevance 19.20

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) transport (TRPV1) plasma membrane (TRPV1)
lipid metabolic process (TRPV1)
Anatomy Link Frequency
body 4
gastrointestinal system 2
neuronal 2
nerve 2
neurons 2
TRPV1 (Homo sapiens)
Pain Link Frequency Relevance Heat
qutenza 118 100.00 Very High Very High Very High
Pain 63 100.00 Very High Very High Very High
Kinase C 25 100.00 Very High Very High Very High
Morphine 12 100.00 Very High Very High Very High
vanilloid receptor subtype 1 9 100.00 Very High Very High Very High
TRP channel 6 100.00 Very High Very High Very High
bradykinin 12 99.98 Very High Very High Very High
Thermal hyperalgesia 6 99.80 Very High Very High Very High
dorsal root ganglion 24 99.72 Very High Very High Very High
Opioid 3 99.70 Very High Very High Very High
Disease Link Frequency Relevance Heat
Pain 44 100.00 Very High Very High Very High
Pruritus 1 100.00 Very High Very High Very High
Irritable Bowel Syndrome /

Irritable Bowel Syndrome Super

1 100.00 Very High Very High Very High
Hyperalgesia 30 99.80 Very High Very High Very High
Ganglion Cysts 27 99.72 Very High Very High Very High
Bordatella Infection 1 98.84 Very High Very High Very High
INFLAMMATION 150 98.48 Very High Very High Very High
Immunization 1 98.08 Very High Very High Very High
Neuropathic Pain 28 96.44 Very High Very High Very High
Hypotension 1 96.28 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Mutation of methionine 547 in S4 of rat TRPV1 to leucine, found in human TRPV1 (M547L), reduced the ability of PPAHV to activate TRPV1 by approximately 20-fold.
Negative_regulation (reduced) of Positive_regulation (activate) of TRPV1
1) Confidence 0.59 Published 2004 Journal J. Biol. Chem. Section Abstract Doc Link 14960593 Disease Relevance 0 Pain Relevance 0.50
In whole-cell patch clamp studies, opioids significantly decreased capsaicin-induced TRPV1 currents in a naloxone- and pertussis toxinsensitive manner.
Negative_regulation (decreased) of Positive_regulation (induced) of TRPV1 associated with bordatella infection, qutenza, narcan and opioid
2) Confidence 0.54 Published 2007 Journal Mol. Pharmacol. Section Abstract Doc Link 17005903 Disease Relevance 1.36 Pain Relevance 1.50
MS reversibly inhibited hTRPV1 activation by polymodal stimuli such as capsaicin, protons, heat, anandamide, and 2-aminoethoxydiphenyl borate.
Negative_regulation (inhibited) of Positive_regulation (activation) of hTRPV1 associated with qutenza
3) Confidence 0.51 Published 2009 Journal Mol. Pharmacol. Section Abstract Doc Link 18987162 Disease Relevance 0.07 Pain Relevance 0.65
We also show that protons decrease the temperature threshold for VR1 activation such that even moderately acidic conditions (pH < or = 5.9) activate VR1 at room temperature.
Negative_regulation (decrease) of Positive_regulation (activation) of VR1
4) Confidence 0.49 Published 1998 Journal Neuron Section Abstract Doc Link 9768840 Disease Relevance 0.25 Pain Relevance 0.44
After application of PAR2 agonists, temperature threshold for TRPV1 activation was reduced from 42 degrees C to well below the body temperature.
Negative_regulation (reduced) of Positive_regulation (activation) of TRPV1 in body associated with agonist
5) Confidence 0.43 Published 2004 Journal J. Neurosci. Section Abstract Doc Link 15128843 Disease Relevance 0.23 Pain Relevance 0.54
Optimization of the heterocyclic A-region led to the design and synthesis of 23, a compound that potently blocked multiple modes of TRPV1 activation.
Negative_regulation (blocked) of Positive_regulation (activation) of TRPV1
6) Confidence 0.43 Published 2007 Journal J. Med. Chem. Section Abstract Doc Link 17585750 Disease Relevance 0.17 Pain Relevance 0.55
We found that BK lowered the threshold temperature for activation of VR1 currents in HEK cells down to well below the physiological body temperature in a concentration-dependent manner through PKC activation.
Negative_regulation (lowered) of Positive_regulation (activation) of VR1 in body associated with kinase c and bradykinin
7) Confidence 0.43 Published 2002 Journal J. Neurophysiol. Section Abstract Doc Link 12091579 Disease Relevance 0.32 Pain Relevance 1.26
Mutation of three highly conserved amino acid residues in the putative sixth transmembrane domain disrupts activation of the VR1 receptor by both capsaicin and resiniferatoxin.
Negative_regulation (disrupts) of Positive_regulation (activation) of VR1 receptor associated with vanilloid receptor subtype 1 and qutenza
8) Confidence 0.43 Published 2001 Journal J. Neurosci. Section Abstract Doc Link 11698581 Disease Relevance 0 Pain Relevance 0.78
Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties.
Negative_regulation (blocking) of Positive_regulation (activation) of TRPV1 receptor associated with qutenza
9) Confidence 0.43 Published 2007 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 17507218 Disease Relevance 0.07 Pain Relevance 0.42
The association of increased keratinocyte TRPV1 in human conditions with pain has recently been demonstrated in women with breast pain, in patients with rectal hypersensitivity and faecal urgency, as well as in pruritic skin of patients with prurigo nodularis.8,23,24 We recently described a patient with steroid-responsive small nerve fibre symptoms of burning feet and hands, where keratinocytes showed strong TRPV1 expression.25 On follow-up skin biopsy after steroid administration, keratinocyte TRPV1 expression was drastically reduced in parallel with remission of clinical symptoms (manuscript in preparation).
Negative_regulation (reduced) of Positive_regulation (increased) of TRPV1 in keratinocytes associated with pain and pruritus
10) Confidence 0.43 Published 2007 Journal Histopathology Section Body Doc Link PMC2121152 Disease Relevance 0.97 Pain Relevance 0.68
Prostaglandins are suggested to reduce the temperature threshold required for TRPV1 activation [30].
Negative_regulation (reduce) of Positive_regulation (activation) of TRPV1
11) Confidence 0.43 Published 2008 Journal Reprod Biol Endocrinol Section Body Doc Link PMC2254422 Disease Relevance 0.81 Pain Relevance 0.84
CONCLUSIONS: It is postulated that Ara C treatment blocked insertion of TRPV1 in the cell membrane, resulting in accumulation of the receptors in the cytoplasm, loss of capsaicin sensitivity, and membrane-bound immunostaining, which was restored with a rebound on withdrawal of Ara C.
Negative_regulation (blocked) of Positive_regulation (insertion) of TRPV1
12) Confidence 0.43 Published 2008 Journal J. Neurooncol. Section Body Doc Link 18414789 Disease Relevance 0.06 Pain Relevance 0
Although rabbit polyclonal antiserum blocked human TRPV1 activation, rabbit monoclonal antibodies (identified on the basis of selective binding to Chinese hamster ovary cells expressing human TRPV1) did not block activation by either capsaicin or protons.
Negative_regulation (blocked) of Positive_regulation (activation) of TRPV1 in ovary associated with qutenza
13) Confidence 0.43 Published 2006 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 16844842 Disease Relevance 0.10 Pain Relevance 0.76
Reversal of capsaicin-induced desensitization by PMA was prevented by a mutation of TRPV1 where phosphorylation sites serine502 and serine800 were replaced with alanine.
Negative_regulation (prevented) of Positive_regulation (mutation) of TRPV1 associated with qutenza
14) Confidence 0.43 Published 2004 Journal Cell Calcium Section Abstract Doc Link 15003856 Disease Relevance 0.07 Pain Relevance 1.10
Since capsaicin-sensitive sensory nerves (rich in TRPV1) are densely distributed in the cardiovascular and gastrointestinal system, activation of TRPV1 either by endogenous ligands or by exogenous agonists has been repeatedly reported to exert hypotensive effects or protective effects against cardiac or gastrointestinal injury through stimulating the synthesis and release of multiple neurotransmitters such as calcitonin gene-related peptide and substance P.
Negative_regulation (distributed) of Positive_regulation (activation) of TRPV1 in gastrointestinal system associated with neurotransmitter, qutenza, injury, hypotension, agonist, substance p and calcitonin gene-related peptide
15) Confidence 0.42 Published 2010 Journal Eur. J. Pharmacol. Section Abstract Doc Link 19879868 Disease Relevance 0.52 Pain Relevance 0.69
Increases in TRPV1 and ROS, generated by synoviocytes in vitro, were reciprocally blocked by TRPV1 antagonists and the ROS scavenger.
Negative_regulation (blocked) of Positive_regulation (Increases) of TRPV1
16) Confidence 0.41 Published 2010 Journal Mol Pain Section Body Doc Link 20691059 Disease Relevance 0 Pain Relevance 0
AMG 9810 is a competitive antagonist of capsaicin activation (IC50 value for human TRPV1, 24.5 +/- 15.7 nM; rat TRPV1, 85.6 +/- 39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294 +/- 192 nM; human TRPV1, 92.7 +/- 72.8 nM), heat (IC50 value for rat TRPV1, 21 +/- 17 nM; human TRPV1, 15.8 +/- 10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine.
Negative_regulation (blocks) of Positive_regulation (activation) of TRPV1 associated with dopamine, qutenza and antagonist
17) Confidence 0.41 Published 2005 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15615864 Disease Relevance 0.24 Pain Relevance 0.73
TRPV1 receptor activation in the esophageal mucosa inhibits esophageal contraction
Negative_regulation (inhibits) of Positive_regulation (activation) of TRPV1 receptor
18) Confidence 0.41 Published 2010 Journal Journal of Neurogastroenterology and Motility Section Body Doc Link PMC2978390 Disease Relevance 0 Pain Relevance 0.23
The rank-order potency of TRPV1 receptor antagonists to inhibit binding of 2 nM [3H]A-778317 correlated well with their functional potencies in blocking TRPV1 receptor activation.
Negative_regulation (blocking) of Positive_regulation (activation) of TRPV1 receptor associated with antagonist and potency
19) Confidence 0.40 Published 2007 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 17660385 Disease Relevance 0.08 Pain Relevance 0.28
The TRPV1 induced increase in COX-2 staining was reduced by pre-treatment with either TRPV1 antagonist capsazepine (5 ?
Negative_regulation (reduced) of Positive_regulation (increase) of TRPV1 associated with antagonist
20) Confidence 0.40 Published 2010 Journal Mol Pain Section Body Doc Link PMC2924298 Disease Relevance 0.21 Pain Relevance 0.25

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