INT73362

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Context Info
Confidence 0.59
First Reported 1998
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 46
Total Number 46
Disease Relevance 8.78
Pain Relevance 17.81

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

transport (Abcb1a) ATPase activity (Abcb1a) plasma membrane (Abcb1a)
transmembrane transport (Abcb1a)
Anatomy Link Frequency
brain 5
blood 2
Caco-2 2
plasma 1
spinal 1
Abcb1a (Mus musculus)
Pain Link Frequency Relevance Heat
tolerance 12 99.98 Very High Very High Very High
methadone 99 99.90 Very High Very High Very High
Opioid 16 99.88 Very High Very High Very High
Spinal cord 25 99.84 Very High Very High Very High
antinociception 23 99.74 Very High Very High Very High
diclofenac 8 99.54 Very High Very High Very High
Morphine 82 99.42 Very High Very High Very High
Nortriptyline 23 99.20 Very High Very High Very High
Antinociceptive 28 99.14 Very High Very High Very High
narcan 1 98.92 Very High Very High Very High
Disease Link Frequency Relevance Heat
Nociception 2 99.84 Very High Very High Very High
Cancer 34 98.98 Very High Very High Very High
Apoptosis 115 98.60 Very High Very High Very High
Carcinoma 18 98.36 Very High Very High Very High
Epilepsy 8 98.24 Very High Very High Very High
Targeted Disruption 31 97.70 Very High Very High Very High
Toxicity 24 97.60 Very High Very High Very High
Sprains And Strains 14 91.16 High High
Liver Cancer 2 89.68 High High
Myeloid Leukemia 101 87.68 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Parallel experiments with R(+)-verapamil, a chemical inhibitor of P-gp, also were performed to further investigate the effect of P-gp on morphine-associated antinociception.
Negative_regulation (inhibitor) of P-gp
1) Confidence 0.59 Published 2000 Journal Pharm. Res. Section Body Doc Link 10955852 Disease Relevance 0 Pain Relevance 0
For example, in vitro studies indicated that fentanyl is a P-gp inhibitor while in vivo studies indicated that it is a P-gp substrate.
Negative_regulation (inhibitor) of P-gp
2) Confidence 0.57 Published 2009 Journal J Pharm Sci Section Abstract Doc Link 19370547 Disease Relevance 0.07 Pain Relevance 0.66
Continuing our studies investigating opioids with reduced P-glycoprotein (P-gp) substrate activity, a series of known 3- and 6-hydroxy, -methoxy, and -desoxymorphine analogs was synthesized and analyzed for P-gp substrate activity and opioid binding affinity. 6-Desoxymorphine ( 7) showed high affinity for opioid receptors and did not induce P-gp-mediated ATP hydrolysis.
Negative_regulation (reduced) of P-gp associated with opioid receptor and opioid
3) Confidence 0.57 Published 2008 Journal J. Med. Chem. Section Abstract Doc Link 18311899 Disease Relevance 0 Pain Relevance 0.69
Similarly, mice with a disruption of the Mdr1a gene were more sensitive to systemic morphine and less sensitive to morphine given centrally.
Negative_regulation (disruption) of Mdr1a associated with morphine
4) Confidence 0.57 Published 2001 Journal Nat. Neurosci. Section Abstract Doc Link 11224543 Disease Relevance 0 Pain Relevance 1.11
However, single-dose rifampin treatment increased the brain uptake of verapamil and quinidine in mdr1a(+/+) mice in a dose- and concentration-dependent manner, consistent with P-gp inhibition.
Negative_regulation (inhibition) of P-gp in brain
5) Confidence 0.57 Published 2003 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12721332 Disease Relevance 0 Pain Relevance 0.20
In conclusion, verapamil yielded complete inhibition of P-gp at the blood-brain barrier and CsA had an effect corresponding to about 50% inhibition.
Negative_regulation (inhibition) of P-gp in blood
6) Confidence 0.55 Published 2006 Journal Drug Metabol Drug Interact Section Abstract Doc Link 16841511 Disease Relevance 0.07 Pain Relevance 0.47
For a series of NT doses (2.5, 5, 10, 25, 30 mg/kg, i.p.) inhibition of P-gp with cyclosporine A (CsA, 200 mg/kg, i.p.) in rats led to NT brain- and liver-serum ratios that were on average 1.3- (p = 0.005) and 2.1- (p = 0.001) fold higher than those of the controls, respectively.
Negative_regulation (inhibition) of P-gp in liver associated with nortriptyline
7) Confidence 0.48 Published 2006 Journal Drug Metabol Drug Interact Section Abstract Doc Link 16841511 Disease Relevance 0.09 Pain Relevance 0.45
RESULTS: Genetic disruption of mdr1a P-gp resulted in 1.3-, 6.6- and 14-fold increases in Clup for morphine, verapamil and quinidine, respectively.
Negative_regulation (disruption) of P-gp
8) Confidence 0.43 Published 2001 Journal Pharm. Res. Section Body Doc Link 11496955 Disease Relevance 0 Pain Relevance 0
Coadministration of a P-gp inhibitor with DPDPE may improve the pharmacologic activity of this opioid peptide.


Negative_regulation (inhibitor) of P-gp
9) Confidence 0.43 Published 1999 Journal Pharm. Res. Section Body Doc Link 10100317 Disease Relevance 0 Pain Relevance 0
RESULTS: Genetic disruption of mdr1a P-gp resulted in 1.3-, 6.6- and 14-fold increases in Clup for morphine, verapamil and quinidine, respectively.
Negative_regulation (disruption) of mdr1a
10) Confidence 0.43 Published 2001 Journal Pharm. Res. Section Body Doc Link 11496955 Disease Relevance 0 Pain Relevance 0
RESULTS: Pharmacologic inhibition of P-gp in monkeys dose-dependently increased brain activity, with a 3.7-fold effect at the highest DCPQ dose (8 mg/kg intravenously).
Negative_regulation (inhibition) of P-gp in brain
11) Confidence 0.42 Published 2008 Journal J. Nucl. Med. Section Body Doc Link 18344435 Disease Relevance 0 Pain Relevance 0
The plasma concentrations of the AMI metabolites and the brain:spleen ratios of AMI, nortriptyline (NOR), 10-OH-AMI and 10-OH-NOR were significantly higher in the -/- mice, demonstrating that AMI and its metabolites are substrates of the P-glycoprotein and that mdr1a activity at the level of the blood-brain barrier reduces the penetration of these substances into the brain.
Negative_regulation (reduces) of mdr1a in brain associated with nortriptyline and endep
12) Confidence 0.39 Published 2000 Journal Neuropsychopharmacology Section Abstract Doc Link 10700657 Disease Relevance 0.16 Pain Relevance 0.95
Furthermore, ABCB4 redistribution was attenuated when PPAR?
Negative_regulation (attenuated) of ABCB4
13) Confidence 0.39 Published 2009 Journal PPAR Research Section Body Doc Link PMC2768028 Disease Relevance 0.28 Pain Relevance 0.11
Efflux studies showed that the loss of morphine from BBCECs was temperature- and energy-dependent and was reduced in the presence of P-gp inhibitors.
Negative_regulation (inhibitors) of P-gp associated with morphine
14) Confidence 0.38 Published 1999 Journal Biochem. Pharmacol. Section Abstract Doc Link 10509747 Disease Relevance 0 Pain Relevance 0.77
These observations indicate that morphine is transported by P-gp out of the brain capillary endothelium and that the BBB permeability of morphine may be altered in the presence of P-gp inhibitors.
Negative_regulation (inhibitors) of P-gp in capillary endothelium associated with morphine
15) Confidence 0.38 Published 1999 Journal Biochem. Pharmacol. Section Abstract Doc Link 10509747 Disease Relevance 0 Pain Relevance 0.64
As quinacrine is known to be a substrate for P-glycoprotein multi-drug resistance (MDR) transporters, we circumvented its poor BBB permeability by utilizing MDR0/0 mice that are deficient in mdr1a and mdr1b genes.
Negative_regulation (deficient) of mdr1a
16) Confidence 0.33 Published 2009 Journal PLoS Pathogens Section Abstract Doc Link PMC2777304 Disease Relevance 0.23 Pain Relevance 0
As potent inhibitors of P-gp are in clinical trials to improve access of desirable chemotherapeutic and antibiotic drugs to the central nervous system, we studied the effect of ondansetron in the absence of extrusion by P-gp.
Negative_regulation (inhibitors) of P-gp in central nervous system associated with central nervous system
17) Confidence 0.29 Published 2006 Journal Anesth. Analg. Section Abstract Doc Link 16931690 Disease Relevance 0.28 Pain Relevance 0.37
CONCLUSION: Valspodar increased methadone's bioavailability as consequence of P-gp inhibition, which resulted in an increased analgesic effect of methadone.


Negative_regulation (inhibition) of P-gp
18) Confidence 0.28 Published 2007 Journal Pharm. Res. Section Body Doc Link 17380267 Disease Relevance 0 Pain Relevance 0
PURPOSE: To quantify the in vivo role of P-glycoprotein (P-gp) in the pharmacokinetics of methadone after intravenous and oral administration, using valspodar as a P-gp inhibitor.
Negative_regulation (inhibitor) of P-gp associated with methadone
19) Confidence 0.28 Published 2007 Journal Pharm. Res. Section Abstract Doc Link 17380267 Disease Relevance 0 Pain Relevance 0.17
P-gp knockout mice and wild-type controls were treated with systemic ondansetron in the presence and absence of clinically used P-gp inhibitors.
Negative_regulation (inhibitors) of P-gp associated with targeted disruption
20) Confidence 0.25 Published 2006 Journal Anesth. Analg. Section Abstract Doc Link 16931690 Disease Relevance 0.51 Pain Relevance 0.56

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