[3h]paroxetine and [3h]citalopram as markers of the human brain 5-ht uptake site

[3h]paroxetine and [3h]citalopram as markers of the human brain 5-ht uptake site


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ABSTRACT The binding of [3H]paroxetine and [3H]citalopram to the brain serotonin (5-HT) uptake site was characterized and compared in human hypothalamus, frontal cortex and caudate nucleus.


Our results showed that the binding exclusively related to the 5-HT uptake site (specific or 5-HT displaceable binding) was identical for both [3H]ligands. The selective 5-HT uptake


inhibitor citalopram displayed the highest potency (Ki) in inhibiting the [3H]paroxetine and [3H]citalopram binding, as compared with the values obtained for desipramine and norzimelidine.


This fact is in accordance with the reported blockage of these compounds of the 5-HT uptake. Furthermore, similar Bmax values were obtained for both radioligands in the brain regions under


study, indicating their binding to the same presynaptic membrane protein. These findings give evidence of the suitability of both [3H]paroxetine and [3H]citalopram as markers of the 5-HT


transporter. However, the higher affinity of [3H] paroxetine (10 to 30-fold with respect to [3H]citalopram) confirms that the radiolabelled form of this compound is the best tool for the


study of the 5-HT uptake site available today. ARTICLE PDF AUTHOR INFORMATION AUTHORS AND AFFILIATIONS * Department of Geriatric Medicine, Linköping, Sweden Belén Arranz & Jan Marcusson


* Department of Clinical Chemistry (Hormone Unit), Hospital Princeps d'Espanya, Barcelona, Spain Belén Arranz Authors * Belén Arranz View author publications You can also search for


this author inPubMed Google Scholar * Jan Marcusson View author publications You can also search for this author inPubMed Google Scholar RIGHTS AND PERMISSIONS Reprints and permissions ABOUT


THIS ARTICLE CITE THIS ARTICLE Arranz, B., Marcusson, J. [3H]Paroxetine and [3H]Citalopram as Markers of the Human Brain 5-HT Uptake Site. _Neuropsychopharmacol_ 11, 265 (1994).


https://doi.org/10.1038/sj.npp.1380134 Download citation * Published: 25 July 2003 * Issue Date: 01 December 1994 * DOI: https://doi.org/10.1038/sj.npp.1380134 SHARE THIS ARTICLE Anyone you


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