Synthesis,affinity and specificity of 18F-setoperone,a potential ligand for in-vivo imaging of cortical serotonin receptors |
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| Affiliation: | 1. Department of Chemistry, Graduate University of Advanced Technology, Kerman, Iran;2. Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, India;3. King Fahd University of Petroleum and Minerals Dhahran, Saudi Arabia;4. Department of Biochemistry, Falavarjan Branch, Islamic Azad University, Falavarjan, Iran |
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| Abstract: | 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). |
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