Abstract
The inhibitory effects of the triarylethylene antiestrogens tamoxifen (TAM) and enclomiphene (EC), and of the estrogenic geometric isomer of the latter compound (zuclomiphene, ZC) on the binding and metabolism of standard substrates in the presence of rabbit liver cytochrome P-450 have been studied. In the presence of microsomes at pH 7.4, the triarylethylenes interfered with the binding of β-diethylaminoethyl diphenylpropylacetate (SKF 525-A) and with the N-demethylation of ethylmorphine. Their inhibitory effects were less pronounced on the binding and metabolism (hydroxylation) of aniline. Kinetic studies showed that EC and TAM interfered with SKF 525-A binding by a mixed mechanism. These results suggest that the triarylethylenes affect preferentially the binding of ‘Type I’ substrates with cytochrome P-450.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
