INT5048

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Context Info
Confidence 0.47
First Reported 1992
Last Reported 2010
Negated 0
Speculated 0
Reported most in Body
Documents 55
Total Number 55
Disease Relevance 18.86
Pain Relevance 19.16

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

extracellular space (Edn1) extracellular region (Edn1) cell-cell signaling (Edn1)
cytoplasm (Edn1)
Anatomy Link Frequency
smooth muscle 6
blood vessels 4
plasma 3
chest 2
brain 2
Edn1 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
antagonist 700 100.00 Very High Very High Very High
agonist 364 100.00 Very High Very High Very High
Nerve growth factor 236 100.00 Very High Very High Very High
Spinal cord 41 100.00 Very High Very High Very High
cytokine 13 100.00 Very High Very High Very High
nociceptor 10 100.00 Very High Very High Very High
substance P 9 100.00 Very High Very High Very High
headache 2 99.88 Very High Very High Very High
Pain 54 99.64 Very High Very High Very High
Calcitonin gene-related peptide 651 99.52 Very High Very High Very High
Disease Link Frequency Relevance Heat
Coronary Vasospasm 6 100.00 Very High Very High Very High
Increased Venous Pressure Under Development 126 99.88 Very High Very High Very High
Hypoxia 34 99.88 Very High Very High Very High
Hyperinsulinism 4 99.80 Very High Very High Very High
Microvascular Angina 1 99.76 Very High Very High Very High
Hyperalgesia 23 99.50 Very High Very High Very High
Angina 19 99.36 Very High Very High Very High
Coronary Artery Disease 11 99.36 Very High Very High Very High
INFLAMMATION 59 99.28 Very High Very High Very High
Paralysis 8 99.16 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
To the best of our knowledge, the consequences of this polyvalent and irreversible binding of ET-1 to ETA-receptors for signaling have not been addressed before.
ET-1 Binding (binding) of
1) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0.05 Pain Relevance 0.31
Several classes of low molecular weight ETA-selective or mixed ET-receptor antagonists have been developed primarily on the basis of prevention of the binding of ET-1 to its receptors[4], [5], [6], [19], [20], [21].
ET-1 Binding (binding) of associated with antagonist
2) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0.34 Pain Relevance 0.22
Binding of Rh-ET-1 (16 nM) to smooth muscle (Fig. 6D) was reduced by BQ788 (1 µM; Fig. 6E) and was prevented by presence of either ET-1 (16 nM) or of both BQ788 (1 µM) and BQ123 (1 µM)[2] indicating selective binding to ETA- and ETB-receptors.
Rh-ET-1 Binding (Binding) of in smooth muscle
3) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.46
Thereafter another part of the ET-1 molecule binds to a second distinct binding-site on the receptor (site L).
ET-1 molecule Binding (binds) of
4) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.36
A part of ET-1, and the low molecular weight antagonists, binds with high affinity to one binding site on the receptor (site H).
ET-1 Binding (binds) of associated with antagonist
5) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.38
Binding of ET-1 at site H is dynamic and remains susceptible to competition by the low molecular weight antagonists.
ET-1 Binding (Binding) of associated with antagonist
6) Confidence 0.47 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.37
The affinity (Kd) and density (Bmax) of [I]ET-1 binding in the brain was found to be similar in placebo and morphine-tolerant neonatal rats.
ET-1 Binding (binding) of in brain associated with morphine
7) Confidence 0.42 Published 2004 Journal J. Cardiovasc. Pharmacol. Section Abstract Doc Link 15838326 Disease Relevance 0.08 Pain Relevance 1.15
It seems to us that paralyzed vasculature is a pre-requisite for equal distribution of ET-1 and its effects on permeability.
ET-1 Binding (distribution) of in vasculature associated with paralysis
8) Confidence 0.36 Published 2005 Journal Crit Care Section Body Doc Link PMC1413997 Disease Relevance 0.52 Pain Relevance 0
Recently, ET-1 has been recognized as a proalgesic mediator that is involved in the pathophysiology of many different pain syndromes which range from inflammatory states, complex regional pain syndromes (CRPS), sickle cell disease to cancer.9,15–17 Furthermore, its nociceptive effects are independent from its vasoconstrictive effects.18 Application of ET-1 has been shown to induce nociceptive behavior in rodents, and pain in humans.15,18–21 The results of clinical studies have shown the existence of a correlation between the severity of the pain and plasma levels of endothelins in patients with prostate cancer.22
ET-1 Binding (recognized) of in plasma associated with nociception, sickle cell anemia, complex regional pain syndromes, pain, inflammation, cancer, syndrome and reprotox - general 1
9) Confidence 0.36 Published 2009 Journal Journal of pain research Section Body Doc Link PMC3004627 Disease Relevance 1.94 Pain Relevance 1.06
Endothelin-1 (ET-1) both stimulates nociceptors and sensitizes them to painful stimuli.
Endothelin-1 Binding (sensitizes) of in nociceptors associated with pain and nociceptor
10) Confidence 0.36 Published 2006 Journal Exp. Biol. Med. (Maywood) Section Abstract Doc Link 16741069 Disease Relevance 0.15 Pain Relevance 0.52
Endothelin-1 (ET-1) both stimulates nociceptors and sensitizes them to painful stimuli.
ET-1 Binding (sensitizes) of in nociceptors associated with pain and nociceptor
11) Confidence 0.36 Published 2006 Journal Exp. Biol. Med. (Maywood) Section Abstract Doc Link 16741069 Disease Relevance 0.15 Pain Relevance 0.52
This model explains the lower potency than affinity and the steepness of the concentration-effect relationships of ET-1 when signaling by ETA-receptors is enhanced by cooperativity between the two binding sites of ET-1.
ET-1 Binding (binding) of associated with potency
12) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.42
Once established, binding of Rh-ET-1 persisted after washout of free Rh-ET-1 and was not reversed by BQ123 (1 µM; Fig. 6F) indicating quasi-irreversible receptor-binding of the agonist.
Rh-ET-1 Binding (binding) of associated with agonist
13) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0.05 Pain Relevance 0.41
Ligand-binding studies and analyses of structure-affinity and structure-selectivity relationships previously indicated quasi-irreversible and polyvalent binding of ET-1 to ETA-receptors[2], [5], [15], [17], [44], [45].
ET-1 Binding (binding) of
14) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0.19 Pain Relevance 0.30
We used rhodamine-labeled ET-1 (Rh-ET-1) and two-photon laser scanning microscopy (TPLSM) focusing on the tunica media, to visualize binding of ET-1 to the smooth muscle.
ET-1 Binding (binding) of in smooth muscle
15) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.51
Thus, we show that ET-1 agonist-receptor binding can be visualised in a vital tissue without the need for supra-physiological receptor densities.
ET-1 Binding (binding) of associated with agonist
16) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.49
We tested whether the quasi-irreversible receptor-binding of ET-1 (i) limits reversing effects of the antagonists and (ii) can be selectively dissociated by an endogenous counterbalancing mechanism.


ET-1 Binding (binding) of associated with antagonist
17) Confidence 0.35 Published 2010 Journal PLoS ONE Section Abstract Doc Link PMC2879375 Disease Relevance 0.09 Pain Relevance 0.25
We used imaging to study the effects of CGRP-receptor activation on binding of ET-1 to arterial smooth muscle ETA-receptors.
ET-1 Binding (binding) of in smooth muscle associated with imagery and calcitonin gene-related peptide
18) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.58
Modulation of ET-1/ETA-receptor binding
ET-1 Binding (binding) of
19) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.41
We used rhodamine-labeled ET-1 (Rh-ET-1) and two-photon laser scanning microscopy (TPLSM) focusing on the tunica media, to visualize binding of ET-1 to the smooth muscle.
ET-1 Binding (binding) of in smooth muscle
20) Confidence 0.35 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2879375 Disease Relevance 0 Pain Relevance 0.46

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