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[3H]Paroxetine and [3H]citalopram as markers of the human brain 5-HT uptake site: a comparison study

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Summary

The binding of [3H]paroxetine and [3H]citalopram to the human brain serotonin (5-HT) uptake site has been characterized and compared. Our results reveal that the binding exclusively involved with the 5-HT uptake site is identical for both [3H]ligands. The selective 5-HT uptake inhibitor citalopram displays the highest affinity for this uptake site, as compared with the affinities obtained for desipramine and norzimeldine, which is in accordance with their respective blockage of 5-HT uptake. Similar Bmax values were obtained for both radioligands in the brain regions studied, indicating their binding to the same presynaptic membrane protein. Together these findings suggest that both [3H]paroxetine and [3H]citalopram are good markers of the 5-HT transporter as both bind selectively and with high affinity to the serotonin uptake sites. However, the higher affinity of [3H]paroxetine confirms that this compound is the best radioligand for the 5-HT uptake site available today.

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Author notes

  1. B. Arranz

    Present address: Department of Geriatric Medicine, University of Linköping, Sweden

Authors and Affiliations

  1. Department of Geriatric Medicine, University of Linköping, Sweden

    J. Marcusson

  2. Department of Clinical Chemistry (Hormone Unit), Hospital Prínceps d'Espanya, Barcelona, Spain

    B. Arranz

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  1. B. Arranz
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  2. J. Marcusson
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Arranz, B., Marcusson, J. [3H]Paroxetine and [3H]citalopram as markers of the human brain 5-HT uptake site: a comparison study. J. Neural Transmission 97, 27–40 (1994). https://doi.org/10.1007/BF01277960

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  • DOI: https://doi.org/10.1007/BF01277960

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