INT56870
From wiki-pain
|
|
|
|
|
Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
Following administration of exogenous codeine the biotransformation to morphine is catalyzed by CYP2D6, which exhibits a genetic so-called debrisoquine/sparteine polymorphism which is expressed in two phenotypes, the extensive and poor metaboliser phenotypes. | |||||||||||||||
| |||||||||||||||
|
We investigated the demethylenation of MDMA and dextromethorphan (DEX), as a comparison drug, in reconstituted microsomes expressing the variant CYP2D6 alleles (*)2, (*)10, and (*)17, all of which have been linked to decreased enzyme activity. | |||||||||||||||
| |||||||||||||||
|
In this study, the regional and cellular expression of CYP2D6 transcripts and proteins in postmortem brain tissues of three individuals was analysed. | |||||||||||||||
| |||||||||||||||
|
Cellular localization and regional distribution of CYP2D6 mRNA and protein expression in human brain. | |||||||||||||||
| |||||||||||||||
|
These results provide clear evidence of CYP2D6 expression in certain regions of the CNS and may indicate the role CYP2D6 plays in a number of drug interactions that are of potential clinical importance for neurological diseases. | |||||||||||||||
| |||||||||||||||
|
The O-demethylation ratio of dextromethorphan that expressed CYP2D6 activity in 19 patients receiving fluoxetine fell in the region of the antimode separating the O-demethylation ratio values observed in 208 extensive metabolizers from 15 poor metabolizers of a control group of healthy subjects. | |||||||||||||||
| |||||||||||||||
|
The latter pathway depends on the genetically polymorphic CYP2D6 which is absent in 7% of the white population (PM) and present in the remainder (EM). | |||||||||||||||
| |||||||||||||||
|
CYP2D6, which is present in the liver and presumably also in the brain, is not expressed in subjects who are poor metabolisers of the sparteine/debrisoquine type. | |||||||||||||||
| |||||||||||||||
|
CYP2D6, which is present in the liver and presumably also in the brain, is not expressed in subjects who are poor metabolisers of the sparteine/debrisoquine type. | |||||||||||||||
| |||||||||||||||
|
Expression, purification, biochemical characterization, and comparative function of human cytochrome P450 2D6.1, 2D6.2, 2D6.10, and 2D6.17 allelic isoforms. | |||||||||||||||
| |||||||||||||||
|
Active CYP2D6.1, 2, 10, and 17 holo-enzymes were expressed in vitro and purified to a high degree of homogeneity as confirmed with SDS-polyacrylamide gel electrophoresis, CO-difference spectroscopy, and mass spectral analysis. | |||||||||||||||
| |||||||||||||||
|
The formation of NAPQI from APAP by cDNA-expressed CYP2D6 was examined. | |||||||||||||||
| |||||||||||||||
|
The analgesic effect of codeine is mediated by its metabolite morphine, which is formed by the polymorphically expressed enzyme CYP2D6; therefore poor metabolizers have no analgesia after administration of codeine. | |||||||||||||||
| |||||||||||||||
|
At pharmacological concentrations of S-fluoxetine, S-norfluoxetine formation rates in the bank of microsomes were found to correlate only with CYP2D6 catalytic activity and only expressed CYP2D6 was found to be capable of forming S-norfluoxetine. | |||||||||||||||
| |||||||||||||||
|
In this report, evidence is presented that the O-demethylation of ibogaine observed in human hepatic microsomes is catalyzed primarily by the polymorphically expressed cytochrome P-4502D6 (CYP2D6). | |||||||||||||||
| |||||||||||||||
|
In this report, evidence is presented that the O-demethylation of ibogaine observed in human hepatic microsomes is catalyzed primarily by the polymorphically expressed cytochrome P-4502D6 (CYP2D6). | |||||||||||||||
| |||||||||||||||
|
Endogenous morphine signaling via nitric oxide regulates the expression of CYP2D6 and COMT: autocrine/paracrine feedback inhibition. | |||||||||||||||
| |||||||||||||||
|
Furthermore, exposure of white blood cells to 10(-6) M S-nitroso-N-acetyl-DL-penicillamine (SNAP), a nitric oxide (NO) donor, reduced the expression of CYP2D6 and COMT. | |||||||||||||||
| |||||||||||||||
|
The verification of the microarray data was accomplished via real-time Taqman reverse transcriptase polymerase chain reaction (RT-PCR) focused on CYP2D6 and COMT expression in different blood samples treated with morphine. | |||||||||||||||
| |||||||||||||||
|
The analysis showed similar changes in the expression of CYP2D6 and COMT mRNA. | |||||||||||||||
| |||||||||||||||
|
General Comments
This test has worked.