INT465

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Context Info
Confidence 0.35
First Reported 1979
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 14
Total Number 14
Disease Relevance 3.04
Pain Relevance 4.07

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 (Adrb1) plasma membrane (Adrb1) nucleus (Adrb1)
cytoplasm (Adrb1) signal transducer activity (Adrb1)
Anatomy Link Frequency
brain 2
plasma 1
spinal 1
spinal cord 1
Adrb1 (Mus musculus)
Pain Link Frequency Relevance Heat
agonist 60 100.00 Very High Very High Very High
Clonidine 11 100.00 Very High Very High Very High
MU agonist 2 99.28 Very High Very High Very High
antidepressant 4 98.70 Very High Very High Very High
beta blocker 32 98.48 Very High Very High Very High
withdrawal 18 97.82 Very High Very High Very High
antinociception 4 96.32 Very High Very High Very High
antagonist 11 96.08 Very High Very High Very High
Angina 2 94.80 High High
cerebral cortex 4 94.08 High High
Disease Link Frequency Relevance Heat
Death 33 99.72 Very High Very High Very High
Opiate Addiction 1 98.00 Very High Very High Very High
Hypertension 2 95.36 Very High Very High Very High
Cv General 3 Under Development 1 94.80 High High
Myocardial Infarction 12 94.12 High High
Heart Rate Under Development 58 93.04 High High
Cv Unclassified Under Development 20 91.12 High High
INFLAMMATION 26 89.76 High High
Pain 3 89.00 High High
Syndrome 1 88.88 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
A withdrawal syndrome may occur after termination of almost all types of antihypertensive drugs, but most experience has been with the centrally acting agents and with beta-adrenoreceptor blockers.
beta-adrenoreceptor Binding (been) of associated with withdrawal
1) Confidence 0.35 Published 1979 Journal J Clin Pharmacol Section Abstract Doc Link 39949 Disease Relevance 0.47 Pain Relevance 0.33
Dexmedetomidine, a compound derived from imidazole, has a high affinity for the alpha-2 adrenoreceptor, on which it acts as a potent agonist.
adrenoreceptor Binding (affinity) of associated with agonist
2) Confidence 0.35 Published 2002 Journal Rev Esp Anestesiol Reanim Section Abstract Doc Link 12455321 Disease Relevance 0.23 Pain Relevance 0.30
Cardioprotection with beta-adrenoceptor blockers.
beta-adrenoceptor Binding (Cardioprotection) of
3) Confidence 0.22 Published 2000 Journal Basic Res. Cardiol. Section Title Doc Link 11192352 Disease Relevance 0.67 Pain Relevance 0.40
Alpha-TOC interfered with antidepressant-induced changes of cellular plasma membrane properties and with recycling of beta-AR.
beta-AR Binding (recycling) of in plasma associated with antidepressant
4) Confidence 0.21 Published 2006 Journal Planta Med. Section Abstract Doc Link 17109256 Disease Relevance 0 Pain Relevance 0.56
To what extent do spinal interactions between an alpha-2 adrenoceptor agonist and a mu opioid agonist influence noxiously evoked c-Fos expression in the rat?
adrenoceptor Binding (interactions) of in spinal associated with mu agonist and agonist
5) Confidence 0.14 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 8764375 Disease Relevance 0.26 Pain Relevance 0.33
Competition assays with a series of compounds of known receptor affinity revealed that [3H]L-654,284 selectively binds to a site with all of the characteristics expected of the alpha 2 adrenoceptor.
adrenoceptor Binding (binds) of
6) Confidence 0.10 Published 1988 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 2907099 Disease Relevance 0 Pain Relevance 0.29
Adrenoceptor (AR) stimulation has both immuno-modulating effects and interacts with excitoxic mechanisms in cell populations within the brain [3,9].
Adrenoceptor Binding (interacts) of in brain
7) Confidence 0.09 Published 2010 Journal J Neuroinflammation Section Body Doc Link PMC3017519 Disease Relevance 0.97 Pain Relevance 0.36
These results indicate that in the soluble extract the interaction between the alpha 2-adrenoceptor and the GTP-binding regulator protein is preserved thus providing an interesting model to study the molecular structure of this system.
adrenoceptor Binding (interaction) of
8) Confidence 0.05 Published 1984 Journal Biochem. Biophys. Res. Commun. Section Abstract Doc Link 6324778 Disease Relevance 0 Pain Relevance 0.21
Solubilization of brain alpha-2 adrenoceptor with a zwitterionic detergent: preservation of agonist binding and its sensitivity to GTP.
adrenoceptor Binding (Solubilization) of in brain associated with agonist
9) Confidence 0.04 Published 1984 Journal Biochem. Biophys. Res. Commun. Section Title Doc Link 6324778 Disease Relevance 0 Pain Relevance 0.21
Different experimental studies have demonstrated that bisoprolol fumarate is one of the most selective beta-1 adrenoreceptor blockers, with a 19-fold higher affinity for the beta-1 receptor than for the beta-2 receptor (Wellstein et al 1986; Smith and Teilter 1999).
beta-1 receptor Binding (affinity) of
10) Confidence 0.03 Published 2007 Journal Vascular Health and Risk Management Section Body Doc Link PMC2291328 Disease Relevance 0.44 Pain Relevance 0.10
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated as inhibitors of phenylethanolamine N-methyltransferase (PNMT) and as inhibitors of the binding of clonidine at the alpha(2)-adrenoceptor.
adrenoceptor Binding (binding) of associated with clonidine
11) Confidence 0.02 Published 1999 Journal J. Med. Chem. Section Abstract Doc Link 10464018 Disease Relevance 0 Pain Relevance 0.10
These compounds were found to be selective inhibitors of PNMT due to their decreased affinity for the alpha(2)-adrenoceptor, which was attributed to steric bulk intolerance around the 3-position of 1,2,3,4-tetrahydroisoquinoline (THIQ) at the alpha(2)-adrenoceptor and to the decreased pK(a) of the THIQ amine due to the 3-trifluoromethyl moiety.
adrenoceptor Binding (affinity) of
12) Confidence 0.02 Published 1999 Journal J. Med. Chem. Section Abstract Doc Link 10464018 Disease Relevance 0 Pain Relevance 0.10
The consistent finding that these two alpha(2)-adrenoceptor agonists interact in a supra-additive manner provides strong evidence that dexmedetomidine and ST-91 produce antinociception by acting at different alpha(2)-adrenoceptor subtypes in the spinal cord.
adrenoceptor Binding (interact) of in spinal cord associated with antinociception, agonist and spinal cord
13) Confidence 0.01 Published 2000 Journal Pain Section Abstract Doc Link 10692612 Disease Relevance 0 Pain Relevance 0.49
Synergistic interactions between two alpha(2)-adrenoceptor agonists, dexmedetomidine and ST-91, in two substrains of Sprague-Dawley rats.
adrenoceptor Binding (interactions) of associated with agonist
14) Confidence 0.01 Published 2000 Journal Pain Section Title Doc Link 10692612 Disease Relevance 0 Pain Relevance 0.30

General Comments

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