Search: L773:1879 0712 OR L773:0014 2999
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[3H]GBR 12935 bindi...
[3H]GBR 12935 binding in platelets from poor and extensive cytochrome P-4502D6 metabolizers.
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Norlén, M (author)
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Norström, A (author)
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Spigset, O (author)
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- Allard, Per (author)
- Umeå universitet,Psykiatri
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(creator_code:org_t)
- 1999
- 1999
- English.
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In: European Journal of Pharmacology. - 0014-2999 .- 1879-0712. ; 366:2-3, s. 329-32
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https://urn.kb.se/re...
Abstract
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- 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.
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- art (subject category)
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