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[3H]GBR 12935 binding in platelets from poor and extensive cytochrome P-4502D6 metabolizers.
Umeå University, Faculty of Medicine, Department of Clinical Sciences, Psychiatry.
1999 (English)In: European Journal of Pharmacology, ISSN 0014-2999, E-ISSN 1879-0712, Vol. 366, no 2-3, 329-32 p.Article in journal (Refereed) Published
Abstract [en]

Previous studies have indicated that part of the binding of [3H] [1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride] ([3H]GBR 12935) to human platelets is to a piperazine acceptor site, which might be associated with cytochrome P-450IID6 (CYP4502D6, debrisoquine-4-hydroxylase). Due to mutant CYP4502D6 alleles, 5-10% of Caucasians are poor metabolizers of CYP4502D6 substrates such as debrisoquine and dextromethorphan. In the present study, possible differences in binding characteristics of [3H]GBR 12935 in platelets from CYP4502D6 poor and extensive metabolizers were investigated. The most prominent finding was a gender difference, with males having significantly higher Kd values than females. There were no differences in Bmax. After correction for gender, there was a tendency towards higher Kd values in poor metabolizers than in extensive metabolizers, although the difference was not statistically significant. Whether this finding corresponds to reduced CYP4502D6 activity is a matter of further investigation.

Place, publisher, year, edition, pages
1999. Vol. 366, no 2-3, 329-32 p.
URN: urn:nbn:se:umu:diva-43974PubMedID: 10082215OAI: diva2:417454
Available from: 2011-05-17 Created: 2011-05-17 Last updated: 2011-05-17

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