INT82839

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Context Info
Confidence 0.59
First Reported 1999
Last Reported 2010
Negated 0
Speculated 1
Reported most in Abstract
Documents 61
Total Number 62
Disease Relevance 16.09
Pain Relevance 8.83

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

transport (ABCB1) ATPase activity (ABCB1) plasma membrane (ABCB1)
transmembrane transport (ABCB1)
Anatomy Link Frequency
brain 4
liver 2
colon 2
MDCK 2
intestines 2
ABCB1 (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 26 99.96 Very High Very High Very High
opioid receptor 7 99.74 Very High Very High Very High
diclofenac 5 99.54 Very High Very High Very High
Morphine 28 99.44 Very High Very High Very High
isoflurane 4 99.36 Very High Very High Very High
adenocard 32 98.92 Very High Very High Very High
Bioavailability 21 98.86 Very High Very High Very High
anesthesia 5 98.48 Very High Very High Very High
cINOD 56 98.46 Very High Very High Very High
narcan 10 98.20 Very High Very High Very High
Disease Link Frequency Relevance Heat
Primary Sclerosing Cholangitis 3 99.84 Very High Very High Very High
Tics 18 99.70 Very High Very High Very High
Injury 374 99.48 Very High Very High Very High
Toxicity 71 99.36 Very High Very High Very High
Enterocolitis 2 99.08 Very High Very High Very High
Leukemia 19 98.72 Very High Very High Very High
Apoptosis 317 98.68 Very High Very High Very High
Malignant Neoplastic Disease 14 98.60 Very High Very High Very High
Increased Venous Pressure Under Development 73 98.20 Very High Very High Very High
INFLAMMATION 87 98.18 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
This investigation tested the hypothesis that plasma concentrations and clinical effects of oral and intravenous fentanyl are greater after inhibition of intestinal and brain P-gp, using the P-gp inhibitor quinidine as an in vivo probe.
Negative_regulation (inhibition) of P-gp in brain
1) Confidence 0.59 Published 2004 Journal J Clin Pharmacol Section Abstract Doc Link 14973303 Disease Relevance 0.06 Pain Relevance 0.09
Quinidine had less effect on fentanyl pharmacodynamics, suggesting that if quinidine is an effective inhibitor of brain P-gp, then P-gp appears to have less effect on brain access of fentanyl.
Negative_regulation (inhibitor) of P-gp in brain
2) Confidence 0.59 Published 2004 Journal J Clin Pharmacol Section Abstract Doc Link 14973303 Disease Relevance 0.13 Pain Relevance 0.05
RESULTS: Commercial preparations inhibited P-gp activity, even if to a different extent, while pure harpagoside was almost ineffective.
Negative_regulation (inhibited) of P-gp
3) Confidence 0.58 Published 2009 Journal Phytomedicine Section Body Doc Link 19577448 Disease Relevance 0.14 Pain Relevance 0
However, the secretory permeability of digoxin and Rho 123 was not strongly affected by rhein and danthron, suggesting that inhibition of MDR1 was not responsible for the increased permeation of furosemide.
Negative_regulation (inhibition) of MDR1
4) Confidence 0.57 Published 2007 Journal Eur J Pharm Biopharm Section Abstract Doc Link 17098405 Disease Relevance 0 Pain Relevance 0.08
Respiratory and miotic effects of morphine in healthy volunteers when P-glycoprotein is blocked by quinidine.
Negative_regulation (blocked) of P-glycoprotein in Respiratory associated with morphine
5) Confidence 0.57 Published 2003 Journal Clin. Pharmacol. Ther. Section Title Doc Link 14534517 Disease Relevance 0 Pain Relevance 0.19
CONCLUSIONS: Whereas morphine clearly produced miosis and respiratory depression, pretreatment with quinidine as an inhibitor of P-glycoprotein did not result in an enhancement of central nervous opioid effects in healthy volunteers.


Negative_regulation (inhibitor) of P-glycoprotein in respiratory
6) Confidence 0.57 Published 2003 Journal Clin. Pharmacol. Ther. Section Body Doc Link 14534517 Disease Relevance 0 Pain Relevance 0
Dexloxiglumide absorption window extends from the jejunum to the colon and the drug is a substrate and a weak inhibitor of P-glycoprotein and multidrug resistance protein 1.
Negative_regulation (inhibitor) of P-glycoprotein in colon
7) Confidence 0.57 Published 2006 Journal Clin Pharmacokinet Section Abstract Doc Link 17112294 Disease Relevance 0.39 Pain Relevance 0.37
To this end, we observed that indomethacin and SC236 directly functioned as noncompetitive inhibitors of P-gp, which were manifested as a reduction of P-gp ATPase activity.
Negative_regulation (reduction) of P-gp
8) Confidence 0.57 Published 2009 Journal Mol. Pharmacol. Section Abstract Doc Link 19264847 Disease Relevance 0.24 Pain Relevance 0.08
In a randomized, double-blind, three-way crossover fashion, subjects received 800 mg quinidine for inhibition of P-glycoprotein; 500 mg probenecid for inhibition of other transporters, including organic anion transporter peptide, multidrug resistance-related protein, and organic anion transporter families; or placebo 1 h before the start of M6G administration.
Negative_regulation (inhibition) of P-glycoprotein
9) Confidence 0.57 Published 2004 Journal Anesthesiology Section Body Doc Link 15564947 Disease Relevance 0 Pain Relevance 0
In contrast to its pharmacokinetics humans, methadone has a short elimination half-life, rapid clearance, and low oral bioavailability in dogs and the extent of absorption is not affected by inhibition of CYP3A, p-gp, and gastric acid secretion.
Negative_regulation (inhibition) of p-gp associated with methadone and bioavailability
10) Confidence 0.57 Published 2005 Journal J. Vet. Pharmacol. Ther. Section Abstract Doc Link 16207309 Disease Relevance 0 Pain Relevance 0.68
Inhibition of UGT2B7 by quinidine was also investigated further, because the effects of this compound on morphine pharmacokinetics (a known UGT2B7 substrate) have been ascribed to inhibition of P-glycoprotein.
Negative_regulation (inhibition) of P-glycoprotein associated with morphine
11) Confidence 0.57 Published 2006 Journal Drug Metab. Dispos. Section Abstract Doc Link 16381668 Disease Relevance 0 Pain Relevance 0.20
The mechanism most often implicated is inhibition of P-glycoprotein, of which digoxin is a substrate.
Negative_regulation (inhibition) of P-glycoprotein
12) Confidence 0.57 Published 2010 Journal Prescrire Int Section Abstract Doc Link 20568489 Disease Relevance 0.51 Pain Relevance 0.13
The efflux of [3H][Dmt1]DALDA from Caco-2 cells was temperature-dependent and was inhibited by DEPC, but was not affected by verapamil, an inhibitor of P-glycoprotein.
Negative_regulation (inhibitor) of P-glycoprotein in Caco-2
13) Confidence 0.57 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12490619 Disease Relevance 0 Pain Relevance 0.12
The efflux of the modified prodrug could be inhibited by GF120918 (an inhibitor for P-gp) and cyclosporin A (an inhibitor for P-gp and MRP2).
Negative_regulation (inhibitor) of P-gp
14) Confidence 0.57 Published 2002 Journal Pharm. Res. Section Body Doc Link 12134949 Disease Relevance 0 Pain Relevance 0
However, this is more likely to be related to Pglycoprotein inhibition in the intestines than in the liver.
Negative_regulation (inhibition) of Pglycoprotein in liver
15) Confidence 0.57 Published 2005 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC1661619 Disease Relevance 0.19 Pain Relevance 0
One study revealed that the COXs inhibitors naproxen and indomethacin heptyl ester were able to downregulate P-glycoprotein in human colorectal CACO-2 cell line
Negative_regulation (downregulate) of P-glycoprotein
16) Confidence 0.57 Published 2010 Journal International Journal of Cell Biology Section Body Doc Link PMC2841246 Disease Relevance 0.56 Pain Relevance 0.07
Ritonavir is a potent CYP3A5 isoenzyme and P-gp inhibitor.
Negative_regulation (inhibitor) of P-gp
17) Confidence 0.53 Published 2009 Journal Pharm World Sci Section Abstract Doc Link 19757141 Disease Relevance 0.71 Pain Relevance 0.42
Lopinavir is also a P-gp inhibitor.
Negative_regulation (inhibitor) of P-gp
18) Confidence 0.53 Published 2009 Journal Pharm World Sci Section Abstract Doc Link 19757141 Disease Relevance 0.70 Pain Relevance 0.42
Nevertheless, measuring a reduction in total cellular P-gp content does not indicate that the MDR phenotype has been reversed as only the cell surface-bound portion of P-gp is responsible for drug efflux [43].
Negative_regulation (reduction) of P-gp
19) Confidence 0.50 Published 2010 Journal PLoS ONE Section Body Doc Link PMC2875382 Disease Relevance 0.22 Pain Relevance 0.03
Moreover, inhibition of ABCB1 and ABCG2 was investigated.
Negative_regulation (inhibition) of ABCB1
20) Confidence 0.49 Published 2008 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 18516595 Disease Relevance 0 Pain Relevance 0.12

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