INT68899

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Context Info
Confidence 0.48
First Reported 1997
Last Reported 2010
Negated 3
Speculated 0
Reported most in Abstract
Documents 19
Total Number 19
Disease Relevance 2.33
Pain Relevance 5.73

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
plasma 3
liver 3
1A2 1
CYP1A2 (Homo sapiens)
Pain Link Frequency Relevance Heat
Duloxetine 84 100.00 Very High Very High Very High
Mexiletine 16 100.00 Very High Very High Very High
Potency 3 99.56 Very High Very High Very High
Paracetamol 18 99.18 Very High Very High Very High
methadone 6 98.18 Very High Very High Very High
pregabalin 141 97.68 Very High Very High Very High
alcohol 15 95.16 Very High Very High Very High
sSRI 16 93.20 High High
cINOD 8 92.92 High High
lidocaine 17 91.68 High High
Disease Link Frequency Relevance Heat
Sudden Death 1 100.00 Very High Very High Very High
Endometriosis (extended) 2 98.52 Very High Very High Very High
Breast Cancer 8 97.52 Very High Very High Very High
Colon Cancer 20 95.76 Very High Very High Very High
Ovarian Cancer 6 94.36 High High
Nicotine Addiction 12 89.68 High High
Sleep Disorders 4 86.16 High High
Toxicity 4 80.96 Quite High
Suicidal Behaviour 8 79.16 Quite High
Disorders Of Creatine Metabolism 3 78.56 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Molecular modeling was used to assess the interaction of these agents with the CYP1A2 active site.
CYP1A2 Binding (interaction) of
1) Confidence 0.48 Published 1999 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 10215663 Disease Relevance 0 Pain Relevance 0.79
Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development.
cytochrome P450 1A2 Binding (interact) of in 1A2
2) Confidence 0.42 Published 2009 Journal Curr. Med. Chem. Section Title Doc Link 19754423 Disease Relevance 0 Pain Relevance 0.11
Human cytochrome P450 1A2 (CYP1A2) is one of the major CYPs in the liver ( approximately 13%) and metabolizes about 20% of clinically used drugs.
CYP1A2 Binding (metabolizes) of in liver
3) Confidence 0.37 Published 2009 Journal Curr. Med. Chem. Section Abstract Doc Link 19754423 Disease Relevance 0 Pain Relevance 0
In addition to CYP1A2, CYP2E1 also catalyzed, although to a lesser extent, its formation.
CYP1A2 Binding (formation) of
4) Confidence 0.37 Published 2003 Journal Drug Metab. Dispos. Section Abstract Doc Link 12814970 Disease Relevance 0 Pain Relevance 0
We have previously shown that residue 382 affected CYP1A1 and CYP1A2 specificities with alkoxyresorufins.
CYP1A2 Binding (specificities) of
5) Confidence 0.37 Published 2010 Journal Drug Metab. Dispos. Section Abstract Doc Link 20335269 Disease Relevance 0 Pain Relevance 0
Tolfenamic acid is a potent CYP1A2 inhibitor in vitro but does not interact in vivo: correction for protein binding is needed for data interpretation.
CYP1A2 Neg (not) Binding (interact) of
6) Confidence 0.37 Published 2007 Journal Eur. J. Clin. Pharmacol. Section Title Doc Link 17618427 Disease Relevance 0 Pain Relevance 0.09
Acetaminophen use (p = 0.05), coffee consumption (p = 0.05) and plasma lycopene (p = 0.06) were positively associated with CYP1A2 activity.
CYP1A2 Binding (associated) of in plasma associated with paracetamol
7) Confidence 0.36 Published 1997 Journal Pharmacogenetics Section Abstract Doc Link 9110357 Disease Relevance 0.32 Pain Relevance 0.23
Plasma lutein explained the largest portion of the variance (7%) and was negatively associated with CYP1A2 activity (p < 0.01), as were use of menopausal replacement estrogens (p = 0.04), plasma alpha-tocopherol (p = 0.05) and alcohol consumption (p = < 0.01).
CYP1A2 Binding (associated) of in Plasma associated with endometriosis (extended) and alcohol
8) Confidence 0.36 Published 1997 Journal Pharmacogenetics Section Abstract Doc Link 9110357 Disease Relevance 0.30 Pain Relevance 0.14
A charge interaction between mexiletine and the Asp313 side chain in the CYP1A2 active site was found, and varying degrees of hydrogen bond formation between these three compounds and the CYP1A2 active site were observed.
CYP1A2 Binding (interaction) of associated with mexiletine
9) Confidence 0.36 Published 1999 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 10215663 Disease Relevance 0 Pain Relevance 0.80
Propafenone is mainly metabolized by CYP2D6 to form 5-hydroxypropafenone (5-OHP) and to a minor extent by CYP1A2 and CYP3A4 to form N-depropylpropafenone (N-DPP).
CYP1A2 Binding (metabolized) of
10) Confidence 0.34 Published 2000 Journal J Clin Psychopharmacol Section Abstract Doc Link 10917404 Disease Relevance 0 Pain Relevance 0.13
We found that CYP2D6 catalyzed only cysteine conjugation; CYP1A2 and 3A4 catalyzed only protein binding; CYP2E1 catalyzed both; and CYP1A1, CYP2A6 and CYP2B6 catalyzed neither.
CYP1A2 Binding (binding) of
11) Confidence 0.33 Published 1997 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 9152386 Disease Relevance 0 Pain Relevance 0.46
Human cytochrome P450 1A2 (CYP1A2) is one of the major CYPs in the liver ( approximately 13%) and metabolizes about 20% of clinically used drugs.
cytochrome P450 1A2 Binding (metabolizes) of in liver
12) Confidence 0.33 Published 2009 Journal Curr. Med. Chem. Section Abstract Doc Link 19754423 Disease Relevance 0 Pain Relevance 0
When the selective catalytic activities were examined as potential covariates, 7-ethoxyresorufin O-deethylation (CYP1A2) activity was found to be associated with the low KM enzyme, however, the high KM enzyme(s) could not be identified.
CYP1A2 Binding (associated) of
13) Confidence 0.32 Published 2000 Journal Pharm. Res. Section Body Doc Link 11303964 Disease Relevance 0 Pain Relevance 0
Incubation of racemic and nonracemic MET with CYP3A4 revealed no stereoselectivity for the transformation to EDDP, whereas no EDDP formation was observed with CYP1A2.
CYP1A2 Neg (no) Binding (formation) of associated with methadone
14) Confidence 0.32 Published 2003 Journal Electrophoresis Section Abstract Doc Link 12900870 Disease Relevance 0 Pain Relevance 0.55
Of clinical relevance, duloxetine does not inhibit or induce the CYP3A4 system, but administration of CYP1A2 inhibitors may result in elevated duloxetine concentrations.42 The CYP1A2 inhibitor thioridazine should not be coadministered with duloxetine due to the risk of serious ventricular arrhythmias and sudden death potentially associated with elevated plasma levels of thioridazine.39 Adverse effects on the fetus have been found in animal reproductive studies, rendering duloxetine a Category C agent for women who are pregnant.42
CYP1A2 Binding (associated) of in plasma associated with duloxetine and sudden death
15) Confidence 0.24 Published 2010 Journal Journal of pain research Section Body Doc Link PMC3004640 Disease Relevance 0.50 Pain Relevance 0.74
Moreover, pregabalin dose not exhibit any significant protein binding, has no known drug interactions and, even at high doses, does not interact with CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, or CYP3A4 systems in vivo (Pfizer Inc. 2006).
CYP1A2 Neg (not) Binding (interact) of associated with pregabalin
16) Confidence 0.18 Published 2007 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2654629 Disease Relevance 0.27 Pain Relevance 1.07
On the other hand, it is reported that naringin also inhibits the demethylation (N-demethylation) of caffeine, metabolized by CYPIA2 [125].
CYPIA2 Binding (metabolized) of
17) Confidence 0.18 Published 2008 Journal Nutr Metab (Lond) Section Body Doc Link PMC2584094 Disease Relevance 0.09 Pain Relevance 0.13
The activity of CYP1A2, CYP2A6, CYP2B6, CYP2D6, CYP2E1, CYP3A4, and CYP2C9 was not affected, and only a moderate inhibitory effect on CYP2C19 (by 38%), as well as a moderate increment of UDP-glucuronosyl-transferase 1A1-mediated ethinylestradiol glucuronidation (by 39%), was seen in the presence of ESL in human liver microsomes in vitro.36

In vivo studies

CYP1A2 Binding (activity) of in liver
18) Confidence 0.13 Published 2010 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2987506 Disease Relevance 0.05 Pain Relevance 0.14
Acetaminophen is thus a possible prodrug for GDEPT in conjunction with CYP1A2.

4-Ipomeanol (4-IM; 15a)

CYP1A2 Binding (conjunction) of associated with paracetamol
19) Confidence 0.12 Published 2003 Journal J Biomed Biotechnol Section Body Doc Link PMC179761 Disease Relevance 0.81 Pain Relevance 0.37

General Comments

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