INT15722

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Context Info
Confidence 0.43
First Reported 1985
Last Reported 2008
Negated 0
Speculated 0
Reported most in Abstract
Documents 25
Total Number 25
Disease Relevance 4.83
Pain Relevance 9.65

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

small molecule metabolic process (PPAP2A) plasma membrane (PPAP2A) lipid metabolic process (PPAP2A)
Anatomy Link Frequency
blood 3
CHO 2
plasma 1
striatum 1
neurons 1
PPAP2A (Homo sapiens)
Pain Link Frequency Relevance Heat
Clonidine 43 99.84 Very High Very High Very High
sodium channel 4 99.56 Very High Very High Very High
Pain 52 99.28 Very High Very High Very High
Catecholamine 10 99.20 Very High Very High Very High
antagonist 34 98.92 Very High Very High Very High
noradrenaline 4 98.92 Very High Very High Very High
agonist 70 98.80 Very High Very High Very High
Opioid 1 98.58 Very High Very High Very High
anesthesia 1 95.32 Very High Very High Very High
Potency 4 94.44 High High
Disease Link Frequency Relevance Heat
Thyroid Disease 4 99.84 Very High Very High Very High
Obesity 19 99.60 Very High Very High Very High
Pain 13 99.24 Very High Very High Very High
Myalgia 4 98.46 Very High Very High Very High
Rheumatoid Arthritis 4 90.56 High High
INFLAMMATION 3 89.60 High High
Hypotension 4 89.44 High High
Leukopenia 1 89.36 High High
Stress 17 89.04 High High
Cognitive Disorder 17 88.48 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
For alpha-2 antagonists, the potency order was: yohimbine greater than idazoxan greater than SK&F-86,466 much greater than benextramine; 3) a description of the impact of benextramine (irreversible alpha-1/alpha-2 antagonist) on human fat cell alpha-2 adrenergic receptors and on human fat cell function; the drug inactivates the alpha-2 adrenergic receptors with a minor impact on beta adrenergic receptors and without noticeable alterations of fat cell function as assessed by preservation of beta adrenergic and Al-adenosine receptor-mediated lipolytic responses; and 4) a definition of the relationship existing between alpha-2 adrenergic receptor occupancy, inhibition of adenylate cyclase activity and antilipolysis with full and partial agonists.
Positive_regulation (inactivates) of alpha-2 in fat cell associated with adenocard, antagonist, obesity, agonist and potency
1) Confidence 0.43 Published 1989 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 2566681 Disease Relevance 0.65 Pain Relevance 0.47
Furthermore, phosphatidic acid phosphohydrolase activity assays showed that the bromoenol lactone-sensitive PAP-1 activity was translocated from the cytosolic fraction to the membrane fraction within 2 min of LPS exposure.
Positive_regulation (translocated) of PAP-1
2) Confidence 0.41 Published 2006 Journal J. Biol. Chem. Section Abstract Doc Link 16950767 Disease Relevance 0.06 Pain Relevance 0.06
Alpha-2 adrenergic activation, achieved with 10 microM clonidine or 10 microM epinephrine, substantially reduced the cyclic AMP concentrations in cells stimulated by 100 microM forskolin or 10 microM isoproterenol.
Positive_regulation (activation) of Alpha-2 associated with clonidine
3) Confidence 0.40 Published 1987 Journal Life Sci. Section Abstract Doc Link 3025542 Disease Relevance 0.07 Pain Relevance 0.10
Microneurographic studies during administration of clonidine suggest that alpha-2 agonists produce a dose-related modulation of central sympathetic nerve discharge, but that other mechanisms presumably involving stimulation of inhibitory peripheral presynaptic alpha-2 receptors are also involved in the antihypertensive action of these agents.
Positive_regulation (stimulation) of alpha-2 in sympathetic associated with agonist and clonidine
4) Confidence 0.38 Published 1985 Journal J. Cardiovasc. Pharmacol. Section Abstract Doc Link 2417051 Disease Relevance 0 Pain Relevance 0.28
We show that the LPS-induced up-regulation of COX-2 depends on the activity of the Mg(+2)-dependent phosphatidic acid phosphohydrolase 1 (PAP-1).
Positive_regulation (up-regulation) of PAP-1
5) Confidence 0.38 Published 2006 Journal J. Biol. Chem. Section Abstract Doc Link 16950767 Disease Relevance 0.09 Pain Relevance 0.09
We show that the LPS-induced up-regulation of COX-2 depends on the activity of the Mg(+2)-dependent phosphatidic acid phosphohydrolase 1 (PAP-1).
Positive_regulation (up-regulation) of phosphatidic acid phosphohydrolase 1
6) Confidence 0.33 Published 2006 Journal J. Biol. Chem. Section Abstract Doc Link 16950767 Disease Relevance 0.09 Pain Relevance 0.09
Comparing the EEG changes between baseline, non-painful and painful stimulations as well as waning pain, we found that the increase in beta-2 activity during muscle pain was significant over the extensive areas of the head, whereas a significant increase in alpha-2 activity took place at the posterior part of the head during waning pain following a marked decrease in overt pain.
Positive_regulation (increase) of alpha-2 in head associated with pain and myalgia
7) Confidence 0.30 Published 2001 Journal Exp Brain Res Section Abstract Doc Link 11713631 Disease Relevance 0.57 Pain Relevance 1.69
The alpha-2 activity augmented during the waning pain following a decrease in the overt pain.
Positive_regulation (augmented) of alpha-2 associated with pain
8) Confidence 0.30 Published 2001 Journal Exp Brain Res Section Abstract Doc Link 11713631 Disease Relevance 0.56 Pain Relevance 1.74
For over a decade it has been known that clonidine and alpha-methyldopa lower blood pressure by activating central and peripheral alpha-2-adrenoceptors and prazosin likewise by antagonizing alpha-1-adrenoceptors.
Positive_regulation (activating) of alpha-2-adrenoceptors in blood associated with clonidine
9) Confidence 0.28 Published 1988 Journal Ann. Clin. Res. Section Abstract Doc Link 2905875 Disease Relevance 0.05 Pain Relevance 0.31
Yohimbine alone markedly enhanced 3H-NE secretion, indicating tonic activation of prejunctional alpha-2 adrenoceptors by endogenous released norepinephrine.
Positive_regulation (activation) of alpha-2
10) Confidence 0.17 Published 1987 Journal Curr. Eye Res. Section Abstract Doc Link 3038473 Disease Relevance 0.11 Pain Relevance 0.43
Co-cultures of odontoblasts with trigeminal neurons indicate a clustering of alpha2 and beta2 sodium channel subunits and, at the sites of cell-cell contact, a co-localization of odontoblasts beta2 subunits with peripherin.
Positive_regulation (clustering) of alpha2 in neurons associated with sodium channel
11) Confidence 0.17 Published 2006 Journal J. Biol. Chem. Section Abstract Doc Link 16831873 Disease Relevance 0.16 Pain Relevance 0.53
The alpha 2- and beta-receptor numbers were both slightly increased in hyperthyroidism, but the ratio between the alpha 2- and beta-receptors was unchanged in relation to normal subjects.
Positive_regulation (increased) of alpha 2 associated with thyroid disease
12) Confidence 0.13 Published 1987 Journal Metab. Clin. Exp. Section Abstract Doc Link 2823049 Disease Relevance 0.74 Pain Relevance 0.30
After protamine application, plasma complement C3a, thromboxane B2 (TxB2), prostaglandin F2 alpha (PGF2 alpha) and KH2PGF2 alpha increased significantly, whereas prostacyclin (6-keto-PGF2 alpha) levels did not change.
Positive_regulation (increased) of KH2PGF2 alpha in plasma
13) Confidence 0.13 Published 1991 Journal J. Appl. Physiol. Section Abstract Doc Link 1757364 Disease Relevance 0.18 Pain Relevance 0.10
Concomitant with an enhanced expression of mu-opioid binding sites, the levels of the inhibitory G proteins Gi alpha 1 and Gi alpha 2 were found to be significantly increased.
Positive_regulation (increased) of Gi alpha 2 associated with opioid
14) Confidence 0.09 Published 1994 Journal J. Neurochem. Section Abstract Doc Link 8133263 Disease Relevance 0.25 Pain Relevance 0.15
We measured agonist-stimulated binding of the stable GTP-analog guanosine-5'-O-(3-[35S]thiotriphosphate) ([35S]GTPgammaS) as a functional assay to monitor G-protein activation by recombinant human alpha2-adrenoceptor subtypes alpha2A, alpha2B and alpha2C. (-)-Noradrenaline was a full agonist in all receptors.
Positive_regulation (activation) of alpha2A associated with noradrenaline and agonist
15) Confidence 0.02 Published 1998 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9760042 Disease Relevance 0.06 Pain Relevance 0.51
Expression, purification, characterization, and in wtro activation of proPAP 1 and proPAP 2 from baculovirus infected insect cells
Positive_regulation (activation) of proPAP 2
16) Confidence 0.01 Published 2002 Journal J Insect Sci Section Body Doc Link PMC405832 Disease Relevance 0.22 Pain Relevance 0
Actions of alpha2 adrenoceptor ligands at alpha2A and 5-HT1A receptors: the antagonist, atipamezole, and the agonist, dexmedetomidine, are highly selective for alpha2A adrenoceptors.
Positive_regulation (Actions) of alpha2A associated with antagonist and agonist
17) Confidence 0.01 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Title Doc Link 9750005 Disease Relevance 0 Pain Relevance 0.27
For example, (+/-)-idazoxan was only 3.6-fold selective for h alpha2A versus h5-HT1A but 51-fold selective for r alpha2A versus r5-HT1A receptors.
Positive_regulation (selective) of alpha2A
18) Confidence 0.01 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9750005 Disease Relevance 0 Pain Relevance 0.32
First, in competition binding experiments at h alpha2A and h5-HT1A receptors expressed in CHO cells, several compounds, including the antagonists 1-(2-pyrimidinyl)piperazine (1-PP), (+/-)-idazoxan, benalfocin (SKF 86466), yohimbine and RX 821,002, displayed preference for h alpha2A versus h5-HT1A receptors of only 1.4-, 3.6-, 4-, 10- and 11-fold, respectively (based on differences in pKi values).
Positive_regulation (preference) of alpha2A associated with antagonist
19) Confidence 0.01 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9750005 Disease Relevance 0 Pain Relevance 0.29
In isolated cell membranes, activation of alpha2A- and alpha2C-adrenoceptors did not affect basal enzyme activity, but activation of alpha2B-adrenoceptors stimulated adenylyl cyclase activity.
Positive_regulation (activation) of alpha2A
20) Confidence 0.01 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9371546 Disease Relevance 0.15 Pain Relevance 0.09

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