INT216840

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Context Info
Confidence 0.47
First Reported 2006
Last Reported 2008
Negated 0
Speculated 0
Reported most in Body
Documents 3
Total Number 13
Disease Relevance 5.23
Pain Relevance 4.85

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

signal transduction (Adora2b) plasma membrane (Adora2b) signal transducer activity (Adora2b)
Anatomy Link Frequency
coronary artery 1
hearts 1
embryonic kidney 1
Adora2b (Mus musculus)
Pain Link Frequency Relevance Heat
adenocard 868 100.00 Very High Very High Very High
agonist 777 99.04 Very High Very High Very High
cytokine 34 98.92 Very High Very High Very High
Inflammation 108 98.56 Very High Very High Very High
antagonist 195 98.52 Very High Very High Very High
Potency 288 98.48 Very High Very High Very High
Opioid 23 91.76 High High
Kinase C 12 79.56 Quite High
Pain 23 79.32 Quite High
fibrosis 33 75.28 Quite High
Disease Link Frequency Relevance Heat
INFLAMMATION 119 98.56 Very High Very High Very High
Vasculogenic Impotence 11 98.28 Very High Very High Very High
Cancer 35 97.72 Very High Very High Very High
Necrosis 12 97.48 Very High Very High Very High
Cv Unclassified Under Development 46 97.20 Very High Very High Very High
Infarction 33 96.56 Very High Very High Very High
Injury 12 93.36 High High
Adhesions 11 92.80 High High
Coronary Artery Disease 34 90.76 High High
Erectile Dysfunction 22 88.28 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
All the reported compounds interacted with the hA2B AR, with EC50 ranging from 9 to 34 nM.
A2B Binding (interacted) of
1) Confidence 0.47 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0 Pain Relevance 0.19
128 nM) and an improved binding profile in comparison with NECA and (S)-PHP-NECA in activating A2B AR, (hA1Ki /hA2B EC50?
A2B Binding (binding) of
2) Confidence 0.36 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.08 Pain Relevance 0.36
The authors proved that the effect on cAMP production was mediated by interaction of the reported compounds with the hA2B AR, establishing that the potent AR antagonist CGS15943 was able to cause a dose-dependent decrease of the cAMP production induced by NECA and by the examined structures.
A2B Binding (interaction) of associated with antagonist
3) Confidence 0.36 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0 Pain Relevance 0.22
This indicates that MRE 2029-F20 is 88- and more than 300-fold selective for the A2B over A1, A2A and A3 subtypes, respectively, which means a range of selectivity similar to [3H]MRS 1754 (selectivity of 210-, 260- and 290-fold for A2B over A1, A2A and A3 subtypes, respectively) and slightly better than [3H]OSIP339391 (selectivity of 70-fold for A2B over A1, A2A and A3 subtypes, respectively).

[3H]MRE 2029-F20 bound specifically to the hA2B receptor stably transfected in human embryonic kidney (HEK) 293 cells with KD of 2.8 nM and Bmax of 450 fmol/mg of protein.

A2B Binding (bound) of in embryonic kidney
4) Confidence 0.35 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0 Pain Relevance 0.11
In rabbit hearts, binding of endogenous adenosine to A2B ARs in early reperfusion is a requirement for both IPC and postconditioning to limit infarction [47].
A2B Binding (binding) of in hearts associated with adenocard and infarction
5) Confidence 0.29 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.80 Pain Relevance 0.46
A2B ARs have been generally defined as the “low-affinity ARs,” as their lower affinity for the endogenous ligand, adenosine, and for some typical agonists, such as 5?
A2B Binding (affinity) of associated with adenocard and agonist
6) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.27 Pain Relevance 0.65
The purinergic regulation of epithelial transports and, above all, involvement of the A2B AR subtype in determining secretion stimulation, suggest the possibility of employing A2B AR-specific ligands as potential modulators of ion transport and the parallel flux of water, which can be considered a natural defence system working to “wash away” injuries in the setting of cellular damage or inflammation.
A2B Binding (employing) of associated with inflammation and injury
7) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.87 Pain Relevance 0.57
The described association of A2B AR with pre/postconditioning cardioprotection, along with the documented strong anti-inflammatory role of A2B AR signalling [49], suggests that A2B AR agonists may represent a new group of therapeutics for patients suffering from coronary artery disease.
A2B Binding (association) of in coronary artery associated with coronary artery disease, inflammation and agonist
8) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.88 Pain Relevance 0.41
A2B ARs have been found on practically every cell in most species, and their sequences are highly similar across species.
A2B Binding (found) of
9) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.22 Pain Relevance 0.24
Several ligands for A2B AR have been identified in recent years [62–64].
A2B Binding (ligands) of
10) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.68 Pain Relevance 0.58
-N-ethylcarboxamido function is generally known to favour A2B AR interaction.
A2B Binding (interaction) of
11) Confidence 0.23 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 0.06 Pain Relevance 0.29
As interaction of adenosine with A2B ARs inhibits production of the proinflammatory cytokine tumor necrosis factor (TNF?)
A2B Binding (interaction) of associated with necrosis, adenocard, cancer and cytokine
12) Confidence 0.22 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2583210 Disease Relevance 1.10 Pain Relevance 0.47
Pretreatment of COS7 cells endogenously expressing A2B receptors with the non-selective agonist NECA (1 ?
A2B Binding (receptors) of associated with agonist
13) Confidence 0.13 Published 2007 Journal Purinergic Signal Section Body Doc Link PMC2245999 Disease Relevance 0.26 Pain Relevance 0.27

General Comments

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