INT152

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Context Info
Confidence 0.38
First Reported 1975
Last Reported 2004
Negated 0
Speculated 0
Reported most in Abstract
Documents 31
Total Number 31
Disease Relevance 3.95
Pain Relevance 11.31

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

mRNA binding (MBD2) nucleus (MBD2) DNA binding (MBD2)
cytoplasm (MBD2)
Anatomy Link Frequency
liver 5
MBD2 (Homo sapiens)
Pain Link Frequency Relevance Heat
cocaine 34 100.00 Very High Very High Very High
Morphine 16 100.00 Very High Very High Very High
ketamine 11 100.00 Very High Very High Very High
Paracetamol 60 99.72 Very High Very High Very High
anesthesia 8 99.60 Very High Very High Very High
aspirin 9 99.38 Very High Very High Very High
Mexiletine 8 98.24 Very High Very High Very High
withdrawal 1 97.84 Very High Very High Very High
lidocaine 7 97.76 Very High Very High Very High
fluoxetine 4 96.20 Very High Very High Very High
Disease Link Frequency Relevance Heat
Necrosis 1 99.86 Very High Very High Very High
Aging 7 99.52 Very High Very High Very High
Protein-energy Malnutrition 1 98.56 Very High Very High Very High
Hepatotoxicity 15 96.48 Very High Very High Very High
Body Weight 6 91.00 High High
INFLAMMATION 13 88.76 High High
Hypertrophy 1 86.84 High High
Toxicity 1 85.36 High High
Feminization 1 80.24 Quite High
Hypertension 6 75.00 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
In a subhuman primate animal model (young rhesus monkey) which was akin to the human situation both for protein energy malnutrition and for drug pharmacokinetics it was observed that hepatic aminopyrine demethylase and chloramphenicol glucuronyl transferase activity was diminished.
Negative_regulation (diminished) of demethylase associated with protein-energy malnutrition
1) Confidence 0.38 Published 1990 Journal Dev Pharmacol Ther Section Abstract Doc Link 2129200 Disease Relevance 0.41 Pain Relevance 0.07
Quinidine, a CYP2D6-specific inhibitor, inhibited ibogaine O-demethylase (IC50 = 0.2 microM), whereas other P450 isoform-specific inhibitors did not inhibit this activity.
Negative_regulation (inhibited) of ibogaine O-demethylase
2) Confidence 0.37 Published 1998 Journal Drug Metab. Dispos. Section Abstract Doc Link 9698290 Disease Relevance 0.05 Pain Relevance 0.10
Preincubation of DMED with microsomes and an NADPH generating system prior to ketamine addition had no additional effect on the inhibition of ketamine demethylase activity, thereby implicating the parent compound rather than a DMED metabolite as the inhibitory species.
Negative_regulation (inhibition) of demethylase associated with ketamine
3) Confidence 0.35 Published 1992 Journal Anesthesiology Section Abstract Doc Link 1361312 Disease Relevance 0 Pain Relevance 0.50
A higher dose of cocaine, 60 mg/kg, elevated the SGOT activity and reduced cocaine N-demethylase activity and 4-nitrophenol GT activity in both SHR and WKY rats.
Negative_regulation (reduced) of N-demethylase associated with cocaine
4) Confidence 0.27 Published 1987 Journal Alcohol Drug Res Section Abstract Doc Link 3113443 Disease Relevance 0.34 Pain Relevance 0.53
Ten daily treatments with cocaine diminished the ethyl morphine N-demethylase activity and the cocaine N-demethylase activity in SHR and WKY rats.
Negative_regulation (diminished) of N-demethylase associated with morphine and cocaine
5) Confidence 0.27 Published 1987 Journal Alcohol Drug Res Section Abstract Doc Link 3113443 Disease Relevance 0.40 Pain Relevance 0.53
Ten daily treatments with cocaine diminished the ethyl morphine N-demethylase activity and the cocaine N-demethylase activity in SHR and WKY rats.
Negative_regulation (diminished) of N-demethylase associated with morphine and cocaine
6) Confidence 0.27 Published 1987 Journal Alcohol Drug Res Section Abstract Doc Link 3113443 Disease Relevance 0.40 Pain Relevance 0.50
Methoxyresorufin O-demethylase activity was inhibited 67 +/- 8%, 20 +/- 5%, and 7 +/- 4% by 2 mM mexiletine, lidocaine, and tocainide, respectively.
Negative_regulation (inhibited) of O-demethylase associated with mexiletine and lidocaine
7) Confidence 0.20 Published 1999 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 10215663 Disease Relevance 0 Pain Relevance 0.88
The mean Ki/EC50 ratio was 0.97 for inhibition of aminopyrine demethylase.
Negative_regulation (inhibition) of aminopyrine demethylase associated with anesthesia
8) Confidence 0.16 Published 1993 Journal Can. J. Physiol. Pharmacol. Section Abstract Doc Link 8513433 Disease Relevance 0 Pain Relevance 0.53
Indomethacin O-demethylase activity in human liver microsomes was competitively inhibited by sulfaphenazole, (S)-warfarin, and tolbutamide and was not affected by alpha-naphthoflavone, (S)-mephenytoin, or erythromycin.
Negative_regulation (inhibited) of O-demethylase in liver
9) Confidence 0.12 Published 1998 Journal Drug Metab. Dispos. Section Abstract Doc Link 9492390 Disease Relevance 0.09 Pain Relevance 0.09
Cytochrome P-450-dependent 7-alkoxycoumarin O-dealkylase activity was not affected by a single administration of 480156-S, but the activity, especially the O-demethylase but not the O-depropylase, was suppressed dose-dependently by multiple administrations.
Negative_regulation (suppressed) of O-demethylase
10) Confidence 0.09 Published 1988 Journal Nippon Yakurigaku Zasshi Section Abstract Doc Link 3266606 Disease Relevance 0.29 Pain Relevance 0.16
Fluvoxamine and diphenytriazol inhibited zolmitriptan N-demethylase activity catalyzed by CYP1A2 (K(i)=3.8+/-0.3 and 3.2+/-0.1 microM, respectively).
Negative_regulation (inhibited) of N-demethylase
11) Confidence 0.06 Published 2003 Journal Chem. Biol. Interact. Section Abstract Doc Link 14642738 Disease Relevance 0.07 Pain Relevance 0.10
The results of these studies, though preliminary in nature, indicate clearly that the aryl-induced mixed-function oxidase systems differ significantly from the PB-induced ones in time course of induction, spectral properties, hyroxylase and demethylase activities, CO-inhibition of these reactions and light-reversal of the inhibition.
Negative_regulation (inhibition) of demethylase
12) Confidence 0.05 Published 1975 Journal Adv. Exp. Med. Biol. Section Abstract Doc Link 1155254 Disease Relevance 0 Pain Relevance 0
The results of in vivo and in vitro studies indicate the following mechanisms of the observed interactions: (a) competition for an active site of promazine N-demethylase and sulfoxidase; (b) adaptive changes in cytochrome P-450, produced by chronic treatment with fluoxetine or fluvoxamine; (c) additionally, increases in the sum of concentrations of promazine+ metabolites, produced by fluoxetine and sertraline in vivo, suggest simultaneous inhibition of another, not investigated by us, metabolic pathway of promazine, e.g. hydroxylation.
Negative_regulation (site) of N-demethylase associated with fluoxetine
13) Confidence 0.04 Published 1999 Journal Eur Neuropsychopharmacol Section Abstract Doc Link 10422895 Disease Relevance 0 Pain Relevance 0.49
Benzodiazepines inhibited in a differential degree the N-demethylase activities for morphine and aminopyrine N-demethylation as well as glucuronyltransferase activity for morphine.
Negative_regulation (inhibited) of N-demethylase associated with morphine
14) Confidence 0.03 Published 1984 Journal Res. Commun. Chem. Pathol. Pharmacol. Section Abstract Doc Link 6429801 Disease Relevance 0 Pain Relevance 0.44
Pretreatment of the rats with pharmacologic doses of acetylsalicylic acid, indomethacin, and ketoprofen decreased both the demethylase and hydroxylase activities of rat liver microsomes.
Negative_regulation (decreased) of demethylase in liver associated with aspirin
15) Confidence 0.03 Published 1985 Journal Can. J. Physiol. Pharmacol. Section Abstract Doc Link 4042014 Disease Relevance 0.07 Pain Relevance 0.17
The addition of 1 mM of ibuprofen, indomethacin, ketoprofen, naproxen, and phenylbutazone to rat liver microsomes inhibit both the aminopyrine N-demethylase and p-nitro-anisole O-demethylase activities.
Negative_regulation (inhibit) of demethylase in liver
16) Confidence 0.03 Published 1985 Journal Can. J. Physiol. Pharmacol. Section Abstract Doc Link 4042014 Disease Relevance 0.15 Pain Relevance 0.32
The addition of 1 mM of ibuprofen, indomethacin, ketoprofen, naproxen, and phenylbutazone to rat liver microsomes inhibit both the aminopyrine N-demethylase and p-nitro-anisole O-demethylase activities.
Negative_regulation (inhibit) of N-demethylase in liver
17) Confidence 0.03 Published 1985 Journal Can. J. Physiol. Pharmacol. Section Abstract Doc Link 4042014 Disease Relevance 0.14 Pain Relevance 0.31
Administration of the parenteral nutrition solution as a continuous enteral infusion via a doudenal catheter slightly decreased p-nitroanisole demethylase activity (26%), but had no other significant effects on either cytochrome P450 concentration or on drug conjugating enzyme activities determined in vitro.
Negative_regulation (decreased) of demethylase
18) Confidence 0.02 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8632327 Disease Relevance 0 Pain Relevance 0.53
Cytochrome P450 concentration and oxidative demethylase activity toward p-nitroanisole were decreased in parallel, 47 and 53%, respectively, and UDP-glucuronosyltransferase activity with p-nitrophenol and acetaminophen as the acceptor aglycones was decreased 44 and 25%, respectively in the animals receiving TPN.
Negative_regulation (decreased) of demethylase associated with paracetamol
19) Confidence 0.02 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8632327 Disease Relevance 0 Pain Relevance 0.63
As SAMC pretreatment (50-200 mg/kg) suppressed hepatic cytochrome P450 2E1-dependent N-nitrosodimethylamine demethylase activity significantly in a dose-dependent manner, we suggest that one of its protective mechanisms is inhibition of cytochrome P450 2E1 activity.
Negative_regulation (suppressed) of demethylase
20) Confidence 0.02 Published 1998 Journal Jpn. J. Pharmacol. Section Abstract Doc Link 9829623 Disease Relevance 0.15 Pain Relevance 0.74

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