Neuroimaging of the serotonin reuptake site requires high-affinity ligands.

Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Research Abstract Details 

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Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Abstract Text:

Betina Elfving,Jacob Madsen,Gitte M Knudsen,Betina Elfving,Jacob Madsen,Gitte M Knudsen,

Numerous attempts have been made to develop suitable radiolabeled tracers for positron emission tomography or single photon emission computed tomography imaging of the serotonin transporter (SERT), but most often, negative outcomes are reported. The aim of this study is to define characteristics of a good SERT radioligand and to investigate species differences. We examined seven different selective serotonin reuptake inhibitors (SSRIs) and that except for one all have been previously tested as emission tomography ligands. The outcome of the ligands as emission tomography tracers was compared in relation with receptor density (Bmax) and/or ligand affinity (Kd) in rat and monkey cerebrum and cerebellum (reference region) membranes. [3H]-(S)-Citalopram and [3H]-(+)-McN5652 display statistically significantly lower affinity, whereas [3H]paroxetine displays statistically significantly higher affinity for SERT in monkey cortex when compared with the rat cerebrum. The affinity of [3H]MADAM, [123I]ADAM, and [11C]DASB for SERT obtained with rat cerebrum and monkey cortex are similar. In monkey cortex, Kd and Bmax could not be determined with [3H]fluoxetine. Of the seven SSRIs, [3H]-(S)-citalopram, [3H]MADAM, and [11C]DASB displayed significant specific binding to SERT in monkey cerebellum, with Bmax cortex:cerebellum ratios being 17, 3, and 4, respectively. In rat brain tissue the ratios were 12, 6, and 3, respectively. In conclusion, it can be estimated that imaging of the human SERT in a high-density region requires radioligands with Kd values between 0.03 and a maximum of 0.3 nM (at 37 degrees C). The differential specific cerebellar binding raises the question of the suitability of cerebellum as a reference region for nonspecific binding.

Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Publishing Authors By Initials

B Elfving,J Madsen,GM Knudsen,B Elfving,J Madsen,GM Knudsen,

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Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Synapse (New York, N.Y.)

VOLUME: 61

Page Numbers: 882-8

Journal Abbreviation: Synapse

ISSN: 0887-4476

DAY: 10

MONTH: Nov

YEAR: 2007

Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Information

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LANGUAGE: eng

NlmUniqueID: 8806914

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Grant and Affiliation Information for Neuroimaging of the serotonin reuptake site requires high-affinity ligands.

AFFILIATION: Neurobiology Research Unit N9201, Rigshospitalet, University Hospital Copenhagen, DK-2100 Copenhagen, Denmark. bef@psykiatri.aaa.dk

Country: United States

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MEDLINETA: Synapse

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