INT65881

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Context Info
Confidence 0.76
First Reported 1996
Last Reported 2010
Negated 3
Speculated 1
Reported most in Abstract
Documents 21
Total Number 22
Disease Relevance 1.19
Pain Relevance 4.57

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small molecule metabolic process (CYP2C19) oxidoreductase activity (CYP2C19) endoplasmic reticulum (CYP2C19)
enzyme binding (CYP2C19)
Anatomy Link Frequency
liver 3
Caco-2 1
1A2 1
body 1
CYP2C19 (Homo sapiens)
Pain Link Frequency Relevance Heat
cINOD 13 99.66 Very High Very High Very High
fluoxetine 42 99.42 Very High Very High Very High
methadone 16 98.08 Very High Very High Very High
Dextromethorphan 1 96.96 Very High Very High Very High
diclofenac 4 95.32 Very High Very High Very High
alcohol 3 93.48 High High
Paracetamol 4 92.80 High High
sSRI 48 84.52 Quite High
Analgesic 6 75.00 Quite High
Opioid 5 75.00 Quite High
Disease Link Frequency Relevance Heat
INFLAMMATION 15 99.54 Very High Very High Very High
Nicotine Addiction 72 97.56 Very High Very High Very High
Headache 7 63.64 Quite High
Rheumatoid Arthritis 52 63.28 Quite High
Body Weight 3 62.20 Quite High
Disease 195 50.00 Quite Low
Depression 52 33.28 Quite Low
Adverse Drug Reaction 13 20.64 Low Low
Diarrhoea 3 19.80 Low Low
Hepatotoxicity 3 19.08 Low Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
While recombinant CYP2C19 and CYP2C9 proteins expressed in yeast or Escherichia coli have been shown to oxidize these agents, the capacity of the corresponding native P450s isolated from human liver to do so is ill defined.
Gene_expression (expressed) of CYP2C19 in liver
1) Confidence 0.76 Published 1998 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 9578596 Disease Relevance 0.10 Pain Relevance 0.10
Despite its tolbutamide hydroxylase activity, the low levels of hepatic CYP2C19 expression (relative to CYP2C9) may preclude an important role for this enzyme in hepatic tolbutamide metabolism and any polymorphisms thereof.
Gene_expression (expression) of CYP2C19
2) Confidence 0.76 Published 1998 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 9578596 Disease Relevance 0 Pain Relevance 0
The KM values were 9.9 +/- 1.2 and 117.1 +/- 13.8 microM and the Vmax values were 0.33 +/- 0.05 and 0.24 +/- 0.04 pmol/min/pmol CYP in microsomes with cDNA-expressed CYP2C9 and CYP2C19, respectively (N = 4).
Gene_expression (expressed) of CYP2C19
3) Confidence 0.76 Published 1998 Journal Drug Metab. Dispos. Section Abstract Doc Link 9492390 Disease Relevance 0 Pain Relevance 0
About 2% of whites are poor metabolizers in whom CYP2C19 is not expressed.
Neg (not) Gene_expression (expressed) of CYP2C19
4) Confidence 0.74 Published 1998 Journal Int Clin Psychopharmacol Section Abstract Doc Link 9817620 Disease Relevance 0 Pain Relevance 0.55
Finally, CYP1A2 and CYP2E1 cDNA-expressed forms of human CYP did not allow PPX formation, CYP2C19 and CYP2D6 produced only small amounts whereas CYP3A4 most efficiently metabolized bupivacaine into PPX.
Gene_expression (produced) of CYP2C19
5) Confidence 0.68 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10725304 Disease Relevance 0 Pain Relevance 0
Expressed CYP2C9, CYP2C19, and CYP2D6 formed R-norfluoxetine following incubation with 1 microM R-fluoxetine and exhibited apparent K(m) values of 9.7, 8.5, and 1.8 microM, respectively.
Gene_expression (Expressed) of CYP2C19 associated with fluoxetine
6) Confidence 0.68 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11356927 Disease Relevance 0 Pain Relevance 0.16
Finally, immunoquantitation revealed that in these human liver samples, expression of CYP2C9 (88. 5 +/- 36 nmol/mg) was 5-fold higher than that of CYP2C19 (17.8 +/- 14 nmol/mg) and nearly 8-fold higher than that of CYP2C8 (11.5 +/- 12 nmol/mg).
Gene_expression (expression) of CYP2C19 in liver
7) Confidence 0.67 Published 1998 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 9578596 Disease Relevance 0 Pain Relevance 0
These transformants are designated Hepc/1A1.4, Hepc/1A2.9, Hepc/2A6L.14, Hepc/2B6.68, Hepc/2C8.46, Hepc/2C9.1, Hepc/2C19.12, Hepc/2D6.39, Hepc/2E1.3-8 and Hepc/3A4.2-30, which stably expressed human CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, respectively.
Gene_expression (expressed) of CYP2C19 in 1A2
8) Confidence 0.66 Published 2001 Journal Toxicol In Vitro Section Abstract Doc Link 11377097 Disease Relevance 0 Pain Relevance 0.10
In contrast, enantiomer interactions were not stereoselective with CYP2C19 or CYP3A4.
Neg (not) Gene_expression (stereoselective) of CYP2C19
9) Confidence 0.65 Published 2007 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 17259447 Disease Relevance 0 Pain Relevance 1.11
Furthermore, rates of norfentanyl production by 10 individual human liver samples were highly correlated (r2 = 0.876, F = 56.46 p < 0.001) with immunochemically determined levels of CYP3A4 present in the samples but not with levels of CYP2C8, CYP2C9, CYP2C19, or CYP2E1.
Neg (not) Gene_expression (present) of CYP2C19 in liver
10) Confidence 0.60 Published 1996 Journal Drug Metab. Dispos. Section Abstract Doc Link 8886601 Disease Relevance 0 Pain Relevance 0.33
Fluoxetine substantially inhibited the metabolism of the CYP2C19 substrate (S)-mephenytoin.
Gene_expression (metabolism) of CYP2C19 associated with fluoxetine
11) Confidence 0.59 Published 2001 Journal J Clin Psychopharmacol Section Abstract Doc Link 11270912 Disease Relevance 0 Pain Relevance 0.69
Expression of CYP1A2, CYP2C8, CYP2C18, CYP2C19, CYP2D6, CYP3A7, CYP4A11, FMO1, and FMO3 was below the limit of detection (LOD) in all investigated samples (data not shown).


Spec (investigated) Gene_expression (Expression) of CYP2C19
12) Confidence 0.55 Published 2006 Journal Environ Health Perspect Section Body Doc Link PMC1665420 Disease Relevance 0.49 Pain Relevance 0
The levels of other CYP proteins, including CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP2E1, were not affected by eletriptan.
Gene_expression (levels) of CYP2C19
13) Confidence 0.53 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10611140 Disease Relevance 0.06 Pain Relevance 0.16
The drug is widely distributed in the body, with low protein binding and a high volume of distribution (see Table 2).118,119 Following oral absorption, venlafaxine undergoes extensive first-pass hepatic metabolism, where conversion to the active metabolite, desvenlafaxine, occurs via demethylation.157 This reaction is mediated by CYP2D6.120 Desvenlafaxine is further metabolized by CYP3A4.122 Other metabolic pathways for venlafaxine include N-demethylation which is probably mediated by CYP3A4.157 CYP2C9 and CYP2C19 isoenzymes may also be involved in the metabolic pathways of both drugs.121
Gene_expression (isoenzymes) of CYP2C19 in body
14) Confidence 0.52 Published 2010 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2938284 Disease Relevance 0 Pain Relevance 0.18
Six were extensive metabolisers, two were poor metabolisers of debrisoquine (CYP2D6) and two were poor metabolisers of mephenytoin (CYP2C19).
Gene_expression (metabolisers) of CYP2C19
15) Confidence 0.47 Published 2002 Journal Eur. J. Clin. Pharmacol. Section Body Doc Link 11936706 Disease Relevance 0 Pain Relevance 0
For several key enzymes, CYP1A2, CYP2A6, CYP2C19 and CYP2E1, these ratios were particularly low (?
Gene_expression (enzymes) of CYP2C19
16) Confidence 0.42 Published 2008 Journal Proceedings of the Royal Society B: Biological Sciences Section Body Doc Link PMC2367444 Disease Relevance 0 Pain Relevance 0
The following specific assays were investigated: testosterone 6beta-hydroxylation [cytochrome P-450 3A4 (CYP3A4)], coumarin hydroxylation (CYP2A6), (R)-warfarin hydroxylation (CYP1A2), (S)-mephenytoin hydroxylation (CYP2C19), p-nitrophenol hydroxylation (CYP2E1) tolbutamide hydroxylation (CYP2C9), dextromethorphan O-demethylation (CYP2D6), epoxide hydrolase and UDP-glucuronyltransferase (UGT) toward paracetamol (UGT1*6), ethinyloestradiol (UGT1*1), p-nitrophenol (UGT(pl 6.2)), and valproic acid.
Gene_expression (hydroxylation) of CYP2C19 associated with paracetamol and dextromethorphan
17) Confidence 0.39 Published 1999 Journal Drug Metab. Dispos. Section Abstract Doc Link 9929511 Disease Relevance 0 Pain Relevance 0.21
Selected compounds were screened for cytochrome P450 inhibition (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4), metabolic stability (rat and human liver microsomes), and cell-membrane permeability (Caco-2).
Gene_expression (screened) of CYP2C19 in Caco-2
18) Confidence 0.38 Published 2006 Journal ChemMedChem Section Abstract Doc Link 16892345 Disease Relevance 0 Pain Relevance 0.10
IL-6 reduces mRNA expression for several cytochrome (CYP)450 isoenzymes (CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) in vitro, and this is reversed by coincubation with TCZ at clinically relevant concentrations.
Gene_expression (expression) of CYP2C19
19) Confidence 0.36 Published 2010 Journal Drug Design, Development and Therapy Section Body Doc Link PMC2990387 Disease Relevance 0.18 Pain Relevance 0.06
Sublines stably expressing human cytochrome P450 cDNA were established by selection with the neomycin analogue G418. 2.
Gene_expression (expressing) of cytochrome P450 cDNA
20) Confidence 0.28 Published 1996 Journal Xenobiotica Section Abstract Doc Link 9004453 Disease Relevance 0.16 Pain Relevance 0.37

General Comments

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