INT96199

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Context Info
Confidence 0.59
First Reported 2001
Last Reported 2010
Negated 0
Speculated 1
Reported most in Body
Documents 15
Total Number 16
Disease Relevance 1.07
Pain Relevance 2.35

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

carbohydrate metabolic process (PGP)
Anatomy Link Frequency
blood 2
nerve 2
enterocyte 1
leg skin 1
brain 1
PGP (Homo sapiens)
Pain Link Frequency Relevance Heat
fluoxetine 6 98.38 Very High Very High Very High
qutenza 12 98.16 Very High Very High Very High
Bioavailability 198 97.76 Very High Very High Very High
antidepressant 12 93.98 High High
Potency 12 86.48 High High
Quantitative sensory testing 20 80.16 Quite High
rapifen 4 79.36 Quite High
c fibre 12 77.92 Quite High
Taxol 3 65.12 Quite High
Analgesic 15 52.04 Quite High
Disease Link Frequency Relevance Heat
Overactive Bladder 4 97.80 Very High Very High Very High
Cancer 34 93.32 High High
Congenital Anomalies 10 90.40 High High
Neuropathic Pain 48 75.00 Quite High
Channelopathies 4 72.72 Quite High
Toxicity 24 50.00 Quite Low
Pain 36 49.32 Quite Low
Death 5 46.80 Quite Low
Metastasis 3 15.52 Low Low
Apoptosis 11 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
To study possible interactions caused by the newer antidepressants we investigated citalopram, fluoxetine, fluvoxamine, paroxetine, reboxetine, sertraline, and venlafaxine and their major metabolites desmethylcitalopram, norfluoxetine, paroxetine-metabolite (paroxetine-M), desmethylsertraline, N-desmethylvenlafaxine, and O-desmethylvenlafaxine for their ability to inhibit Pgp.
Negative_regulation (inhibit) of Pgp associated with antidepressant and fluoxetine
1) Confidence 0.59 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12649369 Disease Relevance 0 Pain Relevance 0.30
RESULTS: From the tested six H1-receptor blockers, seven beta-adrenergic antagonists, four analgesics, ten diuretics and five quinolons, five drugs inhibited Pgp at therapeutic blood levels and two at somewhat higher concentrations.
Negative_regulation (inhibited) of Pgp in blood
2) Confidence 0.58 Published 2001 Journal Anticancer Res. Section Body Doc Link 11396174 Disease Relevance 0 Pain Relevance 0
Pgp inhibition was studied by a fluorometric assay using calcein-acetoxymethylester as Pgp substrate and two different cell systems: L-MDR1 cells (model for human Pgp) and primary porcine brain capillary endothelial cells (pBCECs, model for the blood-brain barrier).
Negative_regulation (inhibition) of Pgp in blood
3) Confidence 0.43 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12649369 Disease Relevance 0 Pain Relevance 0.30
In L-MDR1 cells fluoxetine, norfluoxetine, fluvoxamine, reboxetine, and paroxetine-M revealed intermediate Pgp inhibition and citalopram, desmethylcitalopram, venlafaxine, and N-desmethylvenlafaxine were only weak inhibitors.
Negative_regulation (inhibition) of Pgp associated with fluoxetine
4) Confidence 0.43 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12649369 Disease Relevance 0 Pain Relevance 0.35
Significant synergism for blocking Pgp could be demonstrated for several drugs.
Negative_regulation (blocking) of Pgp
5) Confidence 0.42 Published 2001 Journal Anticancer Res. Section Body Doc Link 11396174 Disease Relevance 0 Pain Relevance 0
By investigating the pharmacokinetic interactions between diltiazem and its metabolites, and with model PgP inhibitors, identifying the contributions of these alternative mechanisms is likely.
Negative_regulation (inhibitors) of PgP
6) Confidence 0.20 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661603 Disease Relevance 0 Pain Relevance 0.04
It is suggested that Cremophor EL acts as a modulator of the absorption process by inhibiting intestinal PGP.
Negative_regulation (inhibiting) of PGP
7) Confidence 0.11 Published 2007 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2374933 Disease Relevance 0 Pain Relevance 0.03
Cremophor EL may inhibit PGP (p-glycoprotein), a relevant efflux pump which is expressed in high amount in gut, biliary tract and the blood brain barrier, and enzymes like CYP3A which may contribute to first pass metabolism.
Spec (may) Negative_regulation (inhibit) of PGP in brain
8) Confidence 0.09 Published 2007 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2374933 Disease Relevance 0 Pain Relevance 0.15
It has been shown that Cremophor EL, Tween 80, Labrasol, Miglyol polyethoxylated, can inhibit the PGP efflux transporter (p-glycoprotein) (Hugger et al 2002; Shono et al 2004; Cornaire et al 2004) and hereby potentially improve bioavailability of drug molecules being PGP substrates.
Negative_regulation (inhibit) of PGP associated with bioavailability
9) Confidence 0.08 Published 2007 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2374933 Disease Relevance 0 Pain Relevance 0.08
This effect is thought to be primarily though Pgp inhibition (instead of CYP3A4 inhibition) since orange juice mediated reduction in enterocyte CYP3A4 concentrations did not produce a similar increase in bioavailability [17].
Negative_regulation (inhibition) of Pgp in enterocyte associated with bioavailability
10) Confidence 0.08 Published 2007 Journal Nutr J Section Body Doc Link PMC2147024 Disease Relevance 0 Pain Relevance 0.22
However, recent studies have demonstrated the inhibition of Pgp by grapefruit juice both by its down-regulation and inhibition of function [26,27].
Negative_regulation (inhibition) of Pgp
11) Confidence 0.08 Published 2007 Journal Nutr J Section Body Doc Link PMC2147024 Disease Relevance 0 Pain Relevance 0.21
CONCLUSIONS: The decrease of PGP9.5 and TRPV1 immunoreactive nerve fibres in responders to resiniferatoxin (to levels in control tissues) suggests that the increased numbers of nerve fibres in patients with NDO are mainly of sensory origin and express TRPV1.
Negative_regulation (decrease) of PGP9 in nerve
12) Confidence 0.07 Published 2004 Journal BJU Int. Section Body Doc Link 15049988 Disease Relevance 0 Pain Relevance 0
OBJECTIVE: To compare PGP9.5 and transient receptor potential vanilloid receptor (TRPV1) suburothelial immunoreactivity between controls and patients with spinal neurogenic detrusor overactivity (NDO) before and after treatment with intravesical resiniferatoxin, as suburothelial PGP9.5-staining nerve fibres decrease in patients with spinal NDO who respond to intravesical capsaicin, and TRPV1 is present on these suburothelial nerve fibres in normal and overactive human urinary bladder.
Negative_regulation (decrease) of PGP9 in nerve associated with qutenza and overactive bladder
13) Confidence 0.06 Published 2004 Journal BJU Int. Section Abstract Doc Link 15049988 Disease Relevance 0.17 Pain Relevance 0.10
These newly formed complexes were found to be, in general, more cytotoxic and inhibited to a lesser extent the Pgp protein than the original Pgp inhibitor derivatives used as ligands.
Negative_regulation (inhibited) of Pgp
14) Confidence 0.04 Published 2010 Journal Journal of Medicinal Chemistry Section Body Doc Link PMC3018145 Disease Relevance 0.09 Pain Relevance 0.04
In patient leg skin biopsies, PGP 9.5- and TRPV1-immunoreactive IEF were reduced and correlated with A?
Negative_regulation (reduced) of PGP in leg skin
15) Confidence 0.02 Published 2007 Journal BMC Neurol Section Abstract Doc Link PMC1959239 Disease Relevance 0.50 Pain Relevance 0.36
Reduction of PGP 9.5 and TRPV1 IEF showed a significant correlation with leg evoked A?
Negative_regulation (Reduction) of PGP in leg
16) Confidence 0.02 Published 2007 Journal BMC Neurol Section Body Doc Link PMC1959239 Disease Relevance 0.31 Pain Relevance 0.19

General Comments

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