INT22210

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Context Info
Confidence 0.78
First Reported 1989
Last Reported 2010
Negated 0
Speculated 0
Reported most in Abstract
Documents 45
Total Number 45
Disease Relevance 4.95
Pain Relevance 10.66

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 (CYP1A2) oxidoreductase activity (CYP1A2) endoplasmic reticulum (CYP1A2)
enzyme binding (CYP1A2)
Anatomy Link Frequency
liver 7
1A2 2
hepatocytes 1
CYP1A2 (Homo sapiens)
Pain Link Frequency Relevance Heat
monoamine 26 100.00 Very High Very High Very High
lidocaine 13 100.00 Very High Very High Very High
Paracetamol 106 99.92 Very High Very High Very High
Migraine 13 99.52 Very High Very High Very High
Duloxetine 185 99.24 Very High Very High Very High
Triptan 31 99.16 Very High Very High Very High
depression 56 98.36 Very High Very High Very High
diclofenac 2 97.84 Very High Very High Very High
rapifen 9 97.82 Very High Very High Very High
Mexiletine 8 96.16 Very High Very High Very High
Disease Link Frequency Relevance Heat
Lung Cancer 1 99.76 Very High Very High Very High
Sleep Disorders 14 99.68 Very High Very High Very High
Headache 17 99.52 Very High Very High Very High
Toxicity 26 99.40 Very High Very High Very High
Nicotine Addiction 57 99.32 Very High Very High Very High
Schizophrenia 40 98.96 Very High Very High Very High
Cluster Headache 20 98.84 Very High Very High Very High
Depression 66 98.36 Very High Very High Very High
Aneuploidy 4 97.52 Very High Very High Very High
Diabetes Mellitus 3 95.04 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
At 5 mM paracetamol the c-mitosis frequency was 14.4 + or - 5.0% and 19.0 + or - 3.8% in the native and CYP1A2 expressing cell lines, respectively (P<0.05).
Gene_expression (expressing) of CYP1A2 associated with paracetamol
1) Confidence 0.78 Published 1996 Journal Pharmacol. Toxicol. Section Abstract Doc Link 8861779 Disease Relevance 0.14 Pain Relevance 0.82
The spindle disturbing effect was only slightly enhanced by expression of CYP1A2, suggesting that metabolic activation plays only a minor role in this genotoxic effect.
Gene_expression (expression) of CYP1A2
2) Confidence 0.78 Published 1996 Journal Pharmacol. Toxicol. Section Abstract Doc Link 8861779 Disease Relevance 0.15 Pain Relevance 0.69
Paracetamol-induced spindle disturbances in V79 cells with and without expression of human CYP1A2.
Gene_expression (expression) of CYP1A2 associated with paracetamol
3) Confidence 0.78 Published 1996 Journal Pharmacol. Toxicol. Section Title Doc Link 8861779 Disease Relevance 0.09 Pain Relevance 0.67
CYP1A2 was predominantly responsible for 3'-OH-genistein formation since its formation was inhibited (>50%, p < 0.05) by a monoclonal antibody specific for CYP1A2, was correlated with CYP1A2 activities of HLM, and was catalyzed by expressed CYP1A2.
Gene_expression (expressed) of CYP1A2
4) Confidence 0.78 Published 2003 Journal Drug Metab. Dispos. Section Abstract Doc Link 12814970 Disease Relevance 0 Pain Relevance 0
Methylated isoflavones biochanin A, prunetin, and formononetin (10-100 microM) were rapidly converted by HLM and expressed CYP1A2 to more active genistein and daidzein.
Gene_expression (expressed) of CYP1A2
5) Confidence 0.78 Published 2003 Journal Drug Metab. Dispos. Section Abstract Doc Link 12814970 Disease Relevance 0 Pain Relevance 0
The maximum rate of formation of D-617 and norverapamil was determined in the microsomal fraction of 21 human livers which had been previously characterized for the individual expression of various P450 enzymes (CYP1A2, CYP2C, CYP2D6, CYP2E1 and CYP3A3/4) by means of Western blotting.
Gene_expression (expression) of CYP1A2 in livers
6) Confidence 0.71 Published 1993 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8232610 Disease Relevance 0.13 Pain Relevance 0.10
Formation of D-617 was correlated with the expression of CYP3A (r = 0.85; P < 0.001) and CYP1A2 (r = 0.57; P < 0.01) in the microsomal fraction of 21 human livers after incubation with racemic verapamil.
Gene_expression (expression) of CYP1A2 in livers
7) Confidence 0.71 Published 1993 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8232610 Disease Relevance 0 Pain Relevance 0
Incubation of cells transfected with human CYP1A2 (H1A2 MZ cells) with 4-20 mM acetaminophen for 6 hours at 37 degrees C caused extensive cytotoxicity (cell viability <10%).
Gene_expression (transfected) of CYP1A2 associated with paracetamol
8) Confidence 0.68 Published 2000 Journal Cancer Gene Ther. Section Abstract Doc Link 10811468 Disease Relevance 0 Pain Relevance 0.41
In conclusion, the use of acetaminophen as prodrug and CYP1A2 as an activating enzyme is a promising combination for gene-directed enzyme prodrug therapy.
Gene_expression (prodrug) of CYP1A2 associated with paracetamol
9) Confidence 0.68 Published 2000 Journal Cancer Gene Ther. Section Abstract Doc Link 10811468 Disease Relevance 0.27 Pain Relevance 0.45
Spindle disturbing effects in terms of c-mitosis and cytotoxicity of paracetamol were investigated in two Chinese hamster V79 cell lines, one of which (V79MZh1A2) was transfected with human CYP1A2.
Gene_expression (transfected) of CYP1A2 associated with paracetamol
10) Confidence 0.68 Published 1996 Journal Pharmacol. Toxicol. Section Abstract Doc Link 8861779 Disease Relevance 0.09 Pain Relevance 0.40
A series of residues in the substrate recognition regions of CYP1A2 (e.g.
Gene_expression (recognition) of CYP1A2
11) Confidence 0.68 Published 2009 Journal Curr. Med. Chem. Section Abstract Doc Link 19754423 Disease Relevance 0 Pain Relevance 0.12
The conversion of biochanin A to genistein appears to be mainly mediated by CYP1A2 because of the strong correlation between the conversion rates and CYP1A2 activities in HLM.
Gene_expression (activities) of CYP1A2
12) Confidence 0.67 Published 2003 Journal Drug Metab. Dispos. Section Abstract Doc Link 12814970 Disease Relevance 0 Pain Relevance 0.06
It is metabolized mainly by cytochrome P450 (CYP) 2 D 6 and, to a minor extent, by CYP1A2.
Gene_expression (metabolized) of CYP1A2
13) Confidence 0.67 Published 2005 Journal Xenobiotica Section Abstract Doc Link 16192107 Disease Relevance 0.58 Pain Relevance 0.61
Very similar results were obtained in a comparison of cells expressing CYP1A2 and aryl sulfotransferase.
Gene_expression (expressing) of CYP1A2
14) Confidence 0.65 Published 2010 Journal Carcinogenesis Section Body Doc Link PMC2802674 Disease Relevance 0.05 Pain Relevance 0.07
The relative contributions of aryl sulfotransferase and NAT2 to the induction of cytotoxicity and mutagenicity were compared in NER-deficient cells expressing CYP1A2 and either of the phase II enzymes.
Gene_expression (expressing) of CYP1A2
15) Confidence 0.65 Published 2010 Journal Carcinogenesis Section Body Doc Link PMC2802674 Disease Relevance 0 Pain Relevance 0.06
In two cell lines both expressing CYP1A2 and NAT2, but one deficient in NER, 2,6-DMA and 3,5-DMA were cytotoxic and mutagenic at dose levels between 100 ?
Gene_expression (expressing) of CYP1A2
16) Confidence 0.65 Published 2010 Journal Carcinogenesis Section Body Doc Link PMC2802674 Disease Relevance 0.07 Pain Relevance 0.08
CONCLUSION: The present data permit us to conclude that the apparent clearance of lidocaine and MEGX was reduced in diabetic patients compared to normal women, suggesting that GDM inhibits the CYP1A2/CYP3A4 isoforms responsible for the metabolism of this drug and its metabolite.


Gene_expression (isoforms) of CYP1A2
17) Confidence 0.65 Published 2008 Journal Eur. J. Clin. Pharmacol. Section Body Doc Link 18679666 Disease Relevance 0 Pain Relevance 0
A significant association with CM was found for the long allele of monoamine oxidase A 30 bp VNTR and CYP1A2*1F variant.
Gene_expression (allele) of CYP1A2 associated with migraine and monoamine
18) Confidence 0.65 Published 2010 Journal J Headache Pain Section Abstract Doc Link 20213484 Disease Relevance 0.54 Pain Relevance 0.95
CONCLUSION: The present data permit us to conclude that the apparent clearance of lidocaine and MEGX was reduced in diabetic patients compared to normal women, suggesting that GDM inhibits the CYP1A2/CYP3A4 isoforms responsible for the metabolism of this drug and its metabolite.


Gene_expression (/) of CYP1A2
19) Confidence 0.65 Published 2008 Journal Eur. J. Clin. Pharmacol. Section Body Doc Link 18679666 Disease Relevance 0 Pain Relevance 0
Direct (IC(50), K(i)) and time-dependent inhibition (IC(50) shift, K(I)/k(inact)) assays were validated in human liver microsomes with liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis for the following enzyme/substrate/inhibitor combinations: CYP1A2/phenacetin/alpha-naphthoflavone/furafylline, CYP2C8/amodiaquine/montelukast/gemfibrozil-1-O-beta-glucuronide, CYP2C9/diclofenac/sulfaphenazole/tienilic acid, CYP2C19/S-mephenytoin/S-benzylnirvanol/S-fluoxetine, CYP2D6/dextromethorphan/quinidine/paroxetine, and CYP3A4/midazolam/testosterone/ketoconazole/azamulin/verapamil/diltiazem.
Gene_expression (/) of CYP1A2 in liver associated with versed, dextromethorphan, diclofenac and fluoxetine
20) Confidence 0.65 Published 2009 Journal Xenobiotica Section Abstract Doc Link 19255936 Disease Relevance 0 Pain Relevance 0.23

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