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- ISSN: 1872-3128
- E-ISSN: 1874-0758
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Assessment of the Inactivation Potential of Desethylamiodarone on Human CYP1A1
- Source: Drug Metabolism Letters, Volume 4, Issue 1, Jan 2010, p. 9 - 14
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- 01 Jan 2010
Abstract
Desethylamiodarone was reported to inactivate human CYP1A1. To assess this, two protocols were implemented employing dilution and non-dilution of the preincubation mixture. Inactivation studies performed with diluted preincubation mixtures showed no inactivation of CYP1A1 by desethylamiodarone. However there was evidence for a mixed competitive inhibition (competitive and the uncompetitive inhibition constants of 2.1 μM and 9.6 μM, respectively) of CYP1A1 by desethylamiodarone. NADPH addition and/or replenishment were found to be important factors in determining the control activity in inactivation studies.
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