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

作者信息

Arranz B, Marcusson J

机构信息

Department of Geriatric Medicine, University of Linköping, Sweden.

出版信息

J Neural Transm Gen Sect. 1994;97(1):27-40. doi: 10.1007/BF01277960.

DOI:10.1007/BF01277960
PMID:7888147
Abstract

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.

摘要

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