Linked Life Data

16890411

Source:http://linkedlifedata.com/resource/pubmed/id/16890411

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2006-9-12
pubmed:abstractText
There are several different experimental systems for screening of in vitro inhibitory potency of drugs under development. In this study we compared three different types of cytochrome P450 (CYP) inhibition tests: the traditional single substrate assays, the fluorescent probe method with recombinant human CYPs, and a novel n-in-one technique. All major hepatic drug-metabolizing CYPs were included (1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4). Six compounds (sotalol, propranolol, citalopram, fluoxetine, oxazepam and diazepam) were selected for detailed comparisons. The IC50 values of each of these compounds were measured using the three assay types. The inhibitory potencies of these model drugs were generally within the same order of magnitude and followed similar inhibition profiles in all the assay types. Clinically observed inhibitory interactions, or lack thereof, were predictable with all three assays. Comparison of potencies of 'diagnostic' inhibitors revealed also some notable differences between the assays, especially regarding CYP2E1. The potency of inhibitors towards CYP3A4 was dependent on the substrate and reaction measured. Generally all three assays gave reasonably comparable results, although some unexplained differences were also noted.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0928-0987
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
29
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
130-8
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Cytochrome P450 (CYP) inhibition screening: comparison of three tests.
pubmed:affiliation
Department of Pharmacology and Toxicology, University of Oulu, P.O. Box 5000, 90014 Oulu, Finland. miia.turpeinen@oulu.fi
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't