Drug metabolism letters, 2008-01, Vol.2 (1), p.51
2008
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Details
- Autor(en) / Beteiligte
- Titel
- An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes
- Ist Teil von
- Drug metabolism letters, 2008-01, Vol.2 (1), p.51
- Ort / Verlag
- United Arab Emirates
- Erscheinungsjahr
- 2008
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The relationship between time-dependent inactivation (TDI) and IC50 is examined using a consolidated method for evaluating CYP450 inhibition during drug discovery. An IC50 fold-shift of >1.5 indicated significant TDI potency. Further, the "shifted IC50" could be used to estimate, the K(I) and TDI potency ratio k(inact)/K(I) to within 2-fold in most cases.
- Sprache
- Englisch
- Identifikatoren
- eISSN: 1874-0758Titel-ID: cdi_pubmed_primary_19356071
- Format
- –
- Schlagworte
- Aryl Hydrocarbon Hydroxylases - antagonists & inhibitors, Cytochrome P-450 CYP2C9, Cytochrome P-450 CYP2D6 Inhibitors, Cytochrome P-450 CYP3A, Cytochrome P-450 CYP3A Inhibitors, Enzyme Inhibitors - administration & dosage, Enzyme Inhibitors - pharmacology, Humans, Inhibitory Concentration 50, Microsomes, Liver - drug effects, Microsomes, Liver - enzymology, Models, Biological, Time Factors