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[3H]GBR 12935 binding in platelets: a possible association with cytochrome P-450IID6?
Umeå University, Faculty of Medicine, Department of Clinical Sciences, Psychiatry.
1997 (English)In: European Journal of Pharmacology, ISSN 0014-2999, E-ISSN 1879-0712, Vol. 332, no 2, 227-30 p.Article in journal (Refereed) Published
Abstract [en]

The nature of [3H] (1-[2-(diphenylmethoxy)ethyl)-4-(3-phenylpropyl) piperazine dihydrochloride) (GBR 12935) binding to human platelets was investigated. A common property of the inhibitors of this binding was their association with the cytochrome P-450 system. cis-Flupenthixol and (1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-[3-phenylpropyl) piperazine dihydrochloride) (GBR 12909) biphasically inhibited the binding. The fraction of [3H]GBR 12935 binding that was inhibited by low concentrations of cis-flupenthixol was sensitive to protease treatment. [3H]GBR 12935 binding in this fraction was saturable and of high affinity (Kd 4.5 nM). The present results reveal that [3H]GBR 12935 binds to multiple sites in platelets and suggest that part of the binding is associated with cytochrome P-450IID6.

Place, publisher, year, edition, pages
1997. Vol. 332, no 2, 227-30 p.
Identifiers
URN: urn:nbn:se:umu:diva-36492PubMedID: 9286626OAI: oai:DiVA.org:umu-36492DiVA: diva2:354301
Available from: 2010-09-30 Created: 2010-09-30 Last updated: 2011-05-17

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