Local view for "https://dbmi-icode-01.dbmi.pitt.edu/dikb/resource/Evidence/275"
| Predicate | Value (sorted: default) |
|---|---|
| rdfs:label | |
| rdf:type | |
| ?:Evidence_assump_list_id |
"51"
|
| ?:Evidence_enzyme_system | |
| ?:Evidence_type | |
| ?:claim_assumed_valid_for_evidence_application_evidence_1824 | |
| ?:content |
"Enzyme system: human liver microsomes
NADPH added: yes
Quote:
To determine whether preincubation affects the inhibition of human liver microsomal dextromethorphan demethylation activity by paroxetine, we used a two-step incubation scheme in which all of the enzyme assay components, minus substrate, are preincubated with paroxetine...Time-dependent inhibition was demonstrated with an apparent K(I) of 4.85 microM and an apparent k(INACT) value of 0.17 min(-1). Spectral scanning of CYP2D6 with paroxetine yielded an increase in absorbance at 456 nm suggesting paroxetine inactivation of CYP2D6 via the formation of a metabolite intermediate complex.
...In contrast, quinidine and fluoxetine, both of which are inhibitors of CYP2D6 activity, did not exhibit a preincubation-dependent increase in inhibitory potency. These data are consistent with mechanism-based inhibition of CYP2D6 by paroxetine but not by quinidine or fluoxetine."
|
| dc:creator | |
| dc:date |
"06/16/2009 13:05:51"
|
| rdfs:seeAlso |
All properties reside in the graph file:///home/swish/src/ClioPatria/guidelines/dikb.ttl
The resource appears as object in one triple:
{ fluoxetine_permanently_deactivates_catalytic_function_cyp2d6, <http://purl.org/swan/1.2/swan-commons#citesAsRefutingEvidence>, evidence_1824 }