Evaluation of the Novel 5-HT4 Receptor PET Ligand [11C]SB207145 in the Göttingen Minipig | Zendy

Birgitte Rahbek Kornum | Zendy; Nanna Marie Lind | Zendy; Nic Gillings | Zendy; Lisbeth Marner | Zendy; Flemming Littrup Andersen | Zendy; Gitte M. Knudsen | Zendy

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Evaluation of the Novel 5-HT₄ Receptor PET Ligand [¹¹C]SB207145 in the Göttingen Minipig

Author(s) -

Birgitte Rahbek Kornum,

Nanna Marie Lind,

Nic Gillings,

Lisbeth Marner,

Flemming Littrup Andersen,

Gitte M. Knudsen

Publication year - 2008

Publication title -

journal of cerebral blood flow and metabolism

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.167

H-Index - 193

eISSN - 1559-7016

pISSN - 0271-678X

DOI - 10.1038/jcbfm.2008.110

Subject(s) - radioligand , binding potential , receptor , striatum , in vivo , ligand (biochemistry) , radioligand assay , 5 ht receptor , positron emission tomography , human brain , chemistry , binding site , biophysics , biology , serotonin , endocrinology , neuroscience , biochemistry , microbiology and biotechnology , dopamine

This study investigates 5-hydroxytryptamine 4 (5-HT(4)) receptor binding in the minipig brain with positron emission tomography (PET), tissue homogenate-binding assays, and autoradiography in vitro. The cerebral uptake and binding of the novel 5-HT(4) receptor radioligand [(11)C]SB207145 in vivo was modelled and the outcome compared with postmortem receptor binding. Different models for quantification of [(11)C]SB207145 binding were evaluated: One-tissue and two-tissue compartment kinetic modelling, Logan arterial input, and three different reference tissue models. We report that the pig autoradiographic 5-HT(4) receptor distribution resembles the human 5-HT(4) receptor distribution with the highest binding in the striatum and no detectable binding in the cerebellum. We found that in the minipig brain [(11)C]SB207145 follows one-tissue compartment kinetics, and the simplified reference tissue model provides stable and precise estimates of the binding potential in all regions. The binding potentials calculated for striatum, midbrain, and cortex from the PET data were highly correlated with 5-HT(4) receptor concentrations determined in brain homogenates from the same regions, except for hippocampus where PET-measurements significantly underestimate the 5-HT(4) receptor binding, probably because of partial volume effects. This study validates the use of [(11)C]SB207145 as a promising PET radioligand for in vivo brain imaging of the 5-HT(4) receptor in humans.

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