INT216752

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Context Info
Confidence 0.36
First Reported 2006
Last Reported 2008
Negated 1
Speculated 0
Reported most in Body
Documents 17
Total Number 17
Disease Relevance 0.76
Pain Relevance 7.36

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

plasma membrane (ADORA2B) signal transducer activity (ADORA2B)
Anatomy Link Frequency
blood cells 1
ADORA2B (Homo sapiens)
Pain Link Frequency Relevance Heat
adenocard 1756 100.00 Very High Very High Very High
antagonist 653 100.00 Very High Very High Very High
agonist 459 99.68 Very High Very High Very High
Potency 14 97.86 Very High Very High Very High
Inflammation 25 69.12 Quite High
Lasting pain 1 46.12 Quite Low
ischemia 2 41.28 Quite Low
Pain 5 39.60 Quite Low
tolerance 11 37.04 Quite Low
analgesia 5 11.44 Low Low
Disease Link Frequency Relevance Heat
Hypoxia 5 94.50 High High
Glioma 44 93.60 High High
Neuroblastoma 44 93.08 High High
Cancer 11 69.92 Quite High
Diabetes Mellitus 55 69.60 Quite High
Disease 10 69.48 Quite High
INFLAMMATION 36 69.12 Quite High
Neurodegenerative Disease 5 68.24 Quite High
Asthma 36 67.08 Quite High
Pain 6 46.12 Quite Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Radioligand binding studies showed that it binds to recombinant A2B receptors in membranes of stably transfected HEK 293 cells.
A2B Binding (binds) of
1) Confidence 0.36 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0 Pain Relevance 0.30
In contrast, 100 mM NaCl had not shown any effect on binding of the adenosine A2B receptor antagonist radioligand [3H]MRS1754 [9].
adenosine A2B receptor Binding (binding) of associated with adenocard and antagonist
2) Confidence 0.32 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.48
In the present study we investigated the ability of sodium ions to modulate agonist and antagonist binding to the human adenosine A2B receptor.
adenosine A2B receptor Binding (binding) of associated with adenocard, antagonist and agonist
3) Confidence 0.32 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.54
Figure 7Effects of different concentrations of sodium chloride on radioligand binding to recombinant human adenosine A2B receptors expressed in HEK-293 cell membranes.
adenosine A2B Binding (binding) of associated with adenocard
4) Confidence 0.32 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.18
Sodium shift experiments were performed at human A2B adenosine receptors expressed in HEK-293 cell membranes with 1 nM [3H]PSB-298 and 50 µg of protein
A2B Binding (receptors) of associated with adenocard
5) Confidence 0.29 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.46
Xanthines, including the natural derivatives theophylline and caffeine, are the natural non-selective antagonists of adenosine and they are able to bind to all four adenosine receptor subtypes A1, A2A, A2B and A3 [6].
A2B Binding (bind) of associated with adenocard and antagonist
6) Confidence 0.28 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0 Pain Relevance 0.52
The rank order of potency of typical adenosine ligands with recombinant hA2B receptors was consistent with that typically found for interactions with the A2B subtype and was also similar in peripheral blood cells.
A2B Binding (interactions) of in blood cells associated with adenocard and potency
7) Confidence 0.27 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0 Pain Relevance 0.20
With a kinetic KD value of 25 nM and a KD value of 60 nM obtained in saturation assays, [3H]PSB-298 showed sufficiently high affinity and appropriate kinetic and physicochemical properties to be useful as an adenosine A2B receptor radioligand.
adenosine A2B receptor Binding (radioligand) of associated with adenocard
8) Confidence 0.25 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.43
Figure 1Structures of antagonist radioligands used for adenosine A2B receptor binding assays
adenosine A2B receptor Binding (binding) of associated with adenocard and antagonist
9) Confidence 0.25 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.63
These studies showed that, although [3H]PSB-298 has a somewhat lower affinity for the rodent adenosine A2B receptors than for the human adenosine A2B receptor subtype, it can still be used as an adenosine A2B receptor radioligand for the labeling of rodent adenosine A2B receptors.
adenosine A2B Binding (affinity) of associated with adenocard
10) Confidence 0.25 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0.13 Pain Relevance 0.82
With the new adenosine A2B receptor radioligand, we were now able to directly determine and quantify the adenosine A2B receptor protein in the cell membranes.
adenosine A2B receptor Binding (radioligand) of associated with adenocard
11) Confidence 0.25 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0.19 Pain Relevance 0.45
Figure 6Saturation experiment of [3H]PSB-298 binding to human adenosine A2B receptors recombinantly expressed in HEK-293 cells.
adenosine A2B Binding (binding) of associated with adenocard
12) Confidence 0.25 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.17
Novel antagonist radioligands to A2B adenosine subtype
A2B Binding (radioligands) of associated with adenocard and antagonist
13) Confidence 0.24 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0 Pain Relevance 0.62
In hypoxic, ischaemic or inflamed conditions the intracellular production of adenosine is increased to very high micromolar concentrations and transported across cell membranes by specific agents finally leading to the stepwise activation of all adenosine receptors, including the low-affinity A2B and A3 subtypes [6].
A2B Binding (affinity) of associated with adenocard and hypoxia
14) Confidence 0.24 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096665 Disease Relevance 0.44 Pain Relevance 0.54
In contrast to other recently developed adenosine A2B receptor antagonist radioligands, [3H]PSB-298 has no tendency to bind to plasticware, and it is therefore easy to handle without the necessity of preparing radioligand dilutions in DMSO, including high DMSO concentrations in the assays (as required for [3H]MRS1754) or adding bovine serum albumin (as required for [3H]OSIP339391).
adenosine A2B receptor Neg (no) Binding (bind) of associated with adenocard and antagonist
15) Confidence 0.24 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.30
For these reasons we decided to synthesize PSB-298 in tritiumlabeled form and investigate its usefulness as an antagonist radioligand for adenosine A2B receptor binding studies. [3H]PSB-298 was prepared by catalytic hydrogenation of the corresponding 1-propargyl derivative PSB-297 using tritium gas (see Figure 2).
adenosine A2B receptor Binding (binding) of associated with adenocard and antagonist
16) Confidence 0.24 Published 2006 Journal Purinergic Signal Section Body Doc Link PMC2096648 Disease Relevance 0 Pain Relevance 0.30
A2B adenosine receptors
A2B Binding (receptors) of associated with adenocard
17) Confidence 0.02 Published 2008 Journal Purinergic Signal Section Body Doc Link PMC2721769 Disease Relevance 0 Pain Relevance 0.41

General Comments

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