Synthesis, affinity and specificity of 18F-setoperone, a potential ligand for in-vivo imaging of cortical serotonin receptors.
Setoperone, a piperidine derivative known for its potent serotonin and moderate dopamine receptor blocking properties was labelled with the positron emitter 18F using a nucleophilic substitution on the nitro derivative. The general pattern of the in-vivo and in-vitro rat brain distribution of this new radioligand was consistent with the mapping of serotonin (5HT2) and dopamine (D2) receptors. The cortical binding of 18F-setoperone was selectively inhibited by ketanserin and not by sulpiride. The affinity of the radiofluorinated ligand for the serotonin receptors was in the nanomolar range (Kd = 0.7 nM).
Maziere
B
B
Service Hospitalier Frédéric Joliot, Département de Biologie Hôpital d'Orsay, France.
Crouzel
C
C
Venet
M
M
Stulzaft
O
O
Sanz
G
G
Ottaviani
M
M
Sejourne
C
C
Pascal
O
O
Bisserbe
J C
JC
D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging*; D001923:Brain Chemistry; D005462:Fluorine Radioisotopes; D066298:In Vitro Techniques; D007553:Isotope Labeling; D008297:Male; D011744:Pyrimidinones; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000032:analysis*; D012702:Serotonin Antagonists
D005462:Fluorine Radioisotopes; D011744:Pyrimidinones; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C045359:setoperone