[3H]GBR 12935 binding to human platelet membranes is sensitive to piperazine derivatives but not to dopamine uptake inhibitors

Irit Gordon*, Ronit Weizman, Moshe Rehavi

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

It remains controversial whether blood platelet can be used as a peripheral model for the central presynaptic dopaminergic neurons. We investigated the existence of dopamine transport complex in human blood platetet membranes using the selective dopamine uptake inhibitor [3H]GBR 12935 as a radioligand. In contrast to [3H]GBR 12935 binding to rat striatal dopamine carrier site, the high affinity [3H]GBR 12935 binding to platelet membranes was insensitive to mazindol and other dopamine uptake inhibitors. Piperazine derivatives including GBR 12909 were found to be potent inhibitors of [3H]GBR 12935 binding to platelet membranes. [3H] GBR 12935, piperazine derivative-sensitive binding to platelet membranes was inhibited by increasing sodium concentration. Kinetic experiments revealed that both association and dissociation rates of [3H] GBR 12935 binding were slower to platelet membranes than to striatal membranes. These results indicate that [3H] GBR 12935 binding to platelet membranes is different from the binding of this ligand to the dopamine uptake complex and seems to label a "piperazine acceptor" site which was previously demonstrated in brain and liver membranes.

Original languageEnglish
Pages (from-to)189-199
Number of pages11
JournalLife Sciences
Volume55
Issue number3
DOIs
StatePublished - 1994

Funding

FundersFunder number
Recanati University
Sackler Faculty of Medicine

    Keywords

    • [H]GBR 12935
    • dopamine transporter
    • piperazine derivatives

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