INT4830

Context Info Confidence 0.48 First Reported 1990 Last Reported 2010 Negated 1 Speculated 5 Reported most in Abstract Documents 158 Total Number 163 Disease Relevance 45.11 Pain Relevance 84.20

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

Anatomy Link Frequency neurons 11 dorsal root ganglion 7 afferent neurons 6 nociceptors 5 CHO 3 Trpv1 (Rattus norvegicus)

Pain Link Frequency Relevance Heat qutenza 2194 100.00 Pain 527 100.00 antagonist 421 100.00 agonist 384 100.00 Calcitonin gene-related peptide 275 100.00 nociceptor 169 100.00 substance P 139 100.00 vanilloid receptor subtype 1 11 100.00 Spinal nerve ligature 7 100.00 Dopamine 18 99.88

Disease Link Frequency Relevance Heat Pain 486 100.00 Fever 32 99.92 Cystitis 6 99.90 Ganglion Cysts 818 99.76 INFLAMMATION 382 99.68 Injury 129 99.36 Stress 13 99.24 Death 34 99.12 Hypersensitivity 44 98.96 Hyperkinesis 3 98.80

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Collectively, the mechanism accounting for the capsaicin-induced increase in the intestinal cefazolin absorption is probably that capsaicin associating with TRPV1 increases the intrinsic permeability of cefazolin in intestine.

TRPV1 Binding (associating) of in intestine associated with qutenza

1) Confidence 0.48 Published 2007 Journal Drug Metab. Pharmacokinet. Section Abstract Doc Link 18159132 Disease Relevance 0 Pain Relevance 0.59

Evodiamine bound to rat TRPV1 with a Ki of 5.95 +/- 0.87 microM, as measured by inhibition of [3H] RTX binding (capsaicin, Ki = 1.8 +/- 0.3 microM).

TRPV1 Binding (bound) of associated with qutenza

2) Confidence 0.48 Published 2004 Journal Org. Biomol. Chem. Section Abstract Doc Link 15305207 Disease Relevance 0 Pain Relevance 0.53

In contrast to its antagonism of vanilloid-induced calcium uptake, IBTU (30 microM) inhibited [3H]resiniferatoxin binding to TRPV1 by less than 10%.

TRPV1 Binding (binding) of

3) Confidence 0.48 Published 2004 Journal Mol. Pharmacol. Section Abstract Doc Link 14742669 Disease Relevance 0 Pain Relevance 0.27

Together these results provide evidence that a synergistic interaction of TRPV1 ligands and elevated temperature activates TRPV1 receptors and results in profound effects on membrane excitability.

TRPV1 Binding (interaction) of

4) Confidence 0.48 Published 2008 Journal Inflamm. Res. Section Abstract Doc Link 18777111 Disease Relevance 0.20 Pain Relevance 0.65

Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1.

TRPV1 Binding (binding) of associated with qutenza and antagonist

5) Confidence 0.48 Published 2005 Journal Mol. Pharmacol. Section Title Doc Link 16135784 Disease Relevance 0 Pain Relevance 0.89

The sensitized TRPV1 channel has heightened responses, and, under these conditions, activators bind the channel with higher affinity.

TRPV1 Binding (bind) of

6) Confidence 0.48 Published 2005 Journal Mol Pain Section Body Doc Link PMC1266034 Disease Relevance 0.21 Pain Relevance 0.84

On a single channel level, acidic pH has been shown to potentiate capsaicin binding to TRPV1 as well as increase channel gating [10].

TRPV1 Binding (binding) of associated with qutenza

7) Confidence 0.48 Published 2005 Journal Mol Pain Section Body Doc Link PMC1266034 Disease Relevance 0.11 Pain Relevance 0.90

The cloned vanilloid receptor-1 (VR1) is recognized as a common molecular target for protons, noxious heat, and vanilloids.

vanilloid receptor-1 Binding (recognized) of

8) Confidence 0.48 Published 2001 Journal Neurosci. Lett. Section Abstract Doc Link 11489540 Disease Relevance 0 Pain Relevance 0.12

The cloned vanilloid receptor-1 (VR1) is recognized as a common molecular target for protons, noxious heat, and vanilloids.

VR1 Binding (recognized) of

9) Confidence 0.48 Published 2001 Journal Neurosci. Lett. Section Abstract Doc Link 11489540 Disease Relevance 0 Pain Relevance 0.12

The cell death induced in a VR1-independent manner has the hallmark of apoptosis, whereas the cell death mediated by vanilloids binding to VR1 is seemingly necrotic.

VR1 Binding (binding) of

10) Confidence 0.48 Published 2000 Journal Chem. Biol. Section Body Doc Link 10903936 Disease Relevance 0 Pain Relevance 0

In conclusion, the present data suggest that local but not IV general anesthetics interact with recombinant rat VR1 receptors with the former anesthetics having antagonistic activity.

VR1 Binding (interact) of

11) Confidence 0.48 Published 2003 Journal Anesth. Analg. Section Abstract Doc Link 12760991 Disease Relevance 0.09 Pain Relevance 0.69

We have examined whether local (lidocaine, prilocaine, and procaine 0.1-10 mM; 10 mM represents 0.25%-0.27% wt/vol) or IV anesthetics (propofol 10 micro M, thiopental 100 micro M, and ketamine 100 micro M) interact with recombinant rat VR1 expressed in human embryonic kidney (HEK293) cells (VR1-HEK293).

VR1 Binding (interact) of in embryonic kidney associated with ketamine and lidocaine

12) Confidence 0.48 Published 2003 Journal Anesth. Analg. Section Abstract Doc Link 12760991 Disease Relevance 0 Pain Relevance 0.52

Specific [3H]resiniferatoxin (RTX) binding detects the vanilloid receptor type I (VR1).

VR1 Binding (binding) of

13) Confidence 0.48 Published 2002 Journal Brain Res. Mol. Brain Res. Section Abstract Doc Link 11834295 Disease Relevance 0.08 Pain Relevance 0.11

Gastro-protective action of lafutidine mediated by capsaicin-sensitive afferent neurons without interaction with TRPV1 and involvement of endogenous prostaglandins.

TRPV1 Binding (interaction) of in afferent neurons associated with qutenza

14) Confidence 0.48 Published 2006 Journal World J. Gastroenterol. Section Title Doc Link 16718783 Disease Relevance 0 Pain Relevance 0.53

[3H]resiniferatoxin binding by the vanilloid receptor: species-related differences, effects of temperature and sulfhydryl reagents.

vanilloid receptor Binding (binding) of associated with inflammation

15) Confidence 0.48 Published 1993 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Title Doc Link 8446186 Disease Relevance 0.15 Pain Relevance 0.54

We have now characterized ligand binding to rat VR1 expressed in human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells and compared the structure-activity relations with those for calcium mobilization.

VR1 Binding (binding) of in CHO

16) Confidence 0.48 Published 1999 Journal Mol. Pharmacol. Section Abstract Doc Link 10462546 Disease Relevance 0.33 Pain Relevance 0.24

All these compounds are lipophilic and therefore bind to the intracellular surface of TRPV1 receptor [26].

TRPV1 receptor Binding (bind) of

17) Confidence 0.48 Published 2010 Journal Mol Pain Section Body Doc Link PMC2959024 Disease Relevance 0.39 Pain Relevance 0.65

CONCLUSIONS: The response to CO(2) perfusion suggests that CO(2) diffuses through the stratum epithelium, interacting with TRPV1 and ASICs in the epithelium or in the submucosa.

TRPV1 Binding (interacting) of in epithelium

18) Confidence 0.48 Published 2008 Journal Gut Section Body Doc Link 18682519 Disease Relevance 0 Pain Relevance 0

The vanilloid receptor VR1 and the vanilloid receptor-like protein VRL-1 are associated with polymodal nociceptors, and may be important for pain processing in normal and injured teeth.

VR1 Binding (associated) of in teeth associated with pain and nociceptor

19) Confidence 0.48 Published 2002 Journal Acta Odontol. Scand. Section Abstract Doc Link 12020118 Disease Relevance 0.18 Pain Relevance 0.24

Co-immunoprecipitation studies were used to demonstrate the physical association of TRPV1 and P2X(3) receptors.

TRPV1 Binding (association) of

20) Confidence 0.47 Published 2009 Journal Pain Section Abstract Doc Link 19223122 Disease Relevance 0.48 Pain Relevance 0.51

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