INT32793

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Context Info
Confidence 0.44
First Reported 1981
Last Reported 2010
Negated 0
Speculated 0
Reported most in Body
Documents 12
Total Number 14
Disease Relevance 1.80
Pain Relevance 5.78

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

Anatomy Link Frequency
spinal 1
smooth muscle 1
brain 1
Slc6a2 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
Dopamine 390 100.00 Very High Very High Very High
Desipramine 18 99.84 Very High Very High Very High
Pain 11 99.60 Very High Very High Very High
Serotonin 31 98.92 Very High Very High Very High
antagonist 72 98.12 Very High Very High Very High
monoamine 26 97.88 Very High Very High Very High
cocaine 23 96.54 Very High Very High Very High
antidepressant 58 95.00 High High
allodynia 1 94.04 High High
fluoxetine 6 93.28 High High
Disease Link Frequency Relevance Heat
Pain 7 99.60 Very High Very High Very High
Shock 2 96.88 Very High Very High Very High
Neuropathic Pain 3 94.04 High High
Targeted Disruption 8 91.36 High High
Urological Neuroanatomy 12 90.68 High High
Parkinson's Disease 13 83.28 Quite High
Death 1 81.68 Quite High
Depression 70 77.24 Quite High
Stress 11 75.00 Quite High
Convulsion 4 75.00 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Several compounds bearing a 3,3-dimethyl group on the indoline ring, 9k, 9o,p, and 9s,t, exhibited potent inhibition of NET (IC(50) = 2.7-6.5 nM) and excellent selectivity over both serotonin and dopamine transporters.
Negative_regulation (inhibition) of NET associated with dopamine and serotonin
1) Confidence 0.44 Published 2010 Journal J. Med. Chem. Section Abstract Doc Link 20131864 Disease Relevance 0 Pain Relevance 0.36
Norepinephrine (NE) amplifies the strength of descending pain inhibition, giving inhibitors of spinal NET clinical utility in the management of pain. chi-MrIA isolated from the venom of a predatory marine snail noncompetitively inhibits NET and reverses allodynia in rat models of neuropathic pain.
Negative_regulation (inhibitors) of NET in spinal associated with pain, allodynia and neuropathic pain
2) Confidence 0.44 Published 2009 Journal J. Med. Chem. Section Abstract Doc Link 19860431 Disease Relevance 0.46 Pain Relevance 0.46
KEY RESULTS: WAY-318068 is a potent and effective inhibitor of the NET with a K(i) of 8.7 nM in a binding assay, and an IC(50) of 6.8 nM in an assay of transporter function, without significant binding to the dopamine transporter.
Negative_regulation (inhibitor) of NET
3) Confidence 0.41 Published 2010 Journal Br. J. Pharmacol. Section Body Doc Link 20590604 Disease Relevance 0 Pain Relevance 0
The second experiment examined the effects of cocaine following the administration of three dose levels of the monoamine antagonists haloperidol, prazosin, yohimbine, propranolol, or metergoline (selected for their ability to block dopamine, alpha-1-norepinephrine, alpha-2-norepinephrine, beta-norepinephrine, and serotonin receptors, respectively).
Negative_regulation (block) of alpha-2-norepinephrine associated with dopamine, antagonist, serotonin, monoamine and cocaine
4) Confidence 0.37 Published 1985 Journal Pharmacol. Biochem. Behav. Section Abstract Doc Link 3991758 Disease Relevance 0.14 Pain Relevance 1.12
The second experiment examined the effects of cocaine following the administration of three dose levels of the monoamine antagonists haloperidol, prazosin, yohimbine, propranolol, or metergoline (selected for their ability to block dopamine, alpha-1-norepinephrine, alpha-2-norepinephrine, beta-norepinephrine, and serotonin receptors, respectively).
Negative_regulation (block) of alpha-1-norepinephrine associated with dopamine, antagonist, serotonin, monoamine and cocaine
5) Confidence 0.37 Published 1985 Journal Pharmacol. Biochem. Behav. Section Abstract Doc Link 3991758 Disease Relevance 0.14 Pain Relevance 1.12
EXPERIMENTAL APPROACH: In this report, we present the in vitro pharmacological and in vivo pharmacokinetic and pharmacological properties of the novel, orally available and CNS penetrant inhibitor of the noradrenaline transporter (NET), WAY-318068 (1-[(1S,2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-7-fluoro-3,3-dimethyl-1,3-dihydro-2H-indol-2-one).
Negative_regulation (inhibitor) of NET
6) Confidence 0.30 Published 2010 Journal Br. J. Pharmacol. Section Body Doc Link 20590604 Disease Relevance 0 Pain Relevance 0
RESULTS: Inflammation was associated with a significant reduction in both beta1-AR and NET density with a positive correlation between the two proteins (r=0.978, p<0.0001).
Negative_regulation (reduction) of NET
7) Confidence 0.28 Published 2009 Journal J Pharm Pharm Sci Section Body Doc Link 20067708 Disease Relevance 0.07 Pain Relevance 0
Various antidepressant drugs (monoamine oxidase inhibitors and tricyclics) enhance norepinephrine availability and lead to adaptive changes in brain noradrenergic systems, namely, decreases in the number of beta receptors and in the responsiveness of adenylate cyclase to norepinephrine monamine oxidase inhibitor, but not after 3 days, there is an increase in norepinephrine release from rat brain microsacs in response to 43 mM KCl stimulation.
Negative_regulation (inhibitor) of norepinephrine monamine oxidase in brain associated with antidepressant and monoamine
8) Confidence 0.12 Published 1982 Journal J. Neurosci. Section Abstract Doc Link 6292376 Disease Relevance 0 Pain Relevance 0.42
Indeed, in the presence of blockade of NET by desipramine, GBR12909 further increased the extracellular concentrations of cortical DA [66].
Negative_regulation (blockade) of NET associated with dopamine and desipramine
9) Confidence 0.06 Published 2010 Journal CNS Neuroscience & Therapeutics Section Body Doc Link PMC2904493 Disease Relevance 0.42 Pain Relevance 1.14
In addition, an important metabolite of quetiapine in humans, norquetiapine, appears to be a blocker of NET (Ki = 58 nM; [139]).
Negative_regulation (blocker) of NET
10) Confidence 0.06 Published 2010 Journal CNS Neuroscience & Therapeutics Section Body Doc Link PMC2904493 Disease Relevance 0.08 Pain Relevance 0.44
Previous studies have shown that blockade of NET together with ?
Negative_regulation (blockade) of NET
11) Confidence 0.06 Published 2010 Journal CNS Neuroscience & Therapeutics Section Body Doc Link PMC2904493 Disease Relevance 0.07 Pain Relevance 0.49
Such a mechanism would directly reduce net hydrogen peroxide levels and superoxide production and increase ATP production.
Negative_regulation (reduce) of net
12) Confidence 0.03 Published 2007 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2654794 Disease Relevance 0.16 Pain Relevance 0.06
The effects of norepinephrine receptor blockade on the deficits of escape behavior induced by haloperidol and by inescapable shock were evaluated.
Negative_regulation (blockade) of norepinephrine receptor associated with shock
13) Confidence 0.00 Published 1981 Journal Psychopharmacology (Berl.) Section Abstract Doc Link 6791235 Disease Relevance 0.25 Pain Relevance 0.13
Presynaptic located alpha 2-adrenoceptors mediate feedback inhibition of norepinephrine-release, while postsynaptic alpha 2-adrenoceptors facilitate smooth muscle contraction in selected vascular beds and stimulate the inhibition of various metabolic processes (insulin and renin secretion, lipolysis).
Negative_regulation (inhibition) of norepinephrine-release in smooth muscle
14) Confidence 0.00 Published 1985 Journal Anaesthesist Section Abstract Doc Link 2983584 Disease Relevance 0 Pain Relevance 0.04

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