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[3H]GBR 12935 binding in platelets from poor and extensive cytochrome P-4502D6 metabolizers.
Umeå universitet, Medicinska fakulteten, Institutionen för klinisk vetenskap, Psykiatri.
1999 (Engelska)Ingår i: European Journal of Pharmacology, ISSN 0014-2999, E-ISSN 1879-0712, Vol. 366, nr 2-3, s. 329-32Artikel i tidskrift (Refereegranskat) 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.

Ort, förlag, år, upplaga, sidor
1999. Vol. 366, nr 2-3, s. 329-32
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URN: urn:nbn:se:umu:diva-43974PubMedID: 10082215OAI: oai:DiVA.org:umu-43974DiVA, id: diva2:417454
Tillgänglig från: 2011-05-17 Skapad: 2011-05-17 Senast uppdaterad: 2018-06-08

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