120th General Meeting of the KCS

Type Symposium
Area Current Trends in Organic Chemistry III: New Reactions and Methodology
Room No. Room 304+305+306
Time FRI 14:30-:
Code ORGN3-1
Subject Development of PET radiotracers for Neurobiological Targets
Authors Sun-Joon Min
Department of Chemical & Molecular Engineering, Hanyang University, Korea
Abstract Serotonin (5-HT) is a major excitatory neurotransmitter that plays an important role in normal physiological conditions. They are mediated by multiple receptor subtypes that have been classified into seven subfamilies (5-HT1-7). Among them, the 5-HT2C is widely distributed in the human brain, in particular, displaying a high density in striatal, cortical, and limbic regions. It has been reported that dysfunction of the 5-HT2C contributed to a variety of brain-related disorders such as schizophrenia, Parkinson’s disease, and anxiety. Up to date, it is difficult to study a direct mechanism of action between the 5-HT2C and such brain diseases due to lack of proper chemical probes. Accordingly, development of an in vivo method for measuring its function and density is important to identify the role of the 5-HT2C receptor in the brain. Thus, PET imagining might be one of the potential tools for this purpose. A number of selective 5-HT2C ligands have been developed, but only a few of them have been evaluated as PET radiotracers. Herein, we describe synthesis and biological evaluation of a pyrimidine derivative as a selective 5-HT2C PET radiotracer. We have successfully developed a synthetic route toward [18F]-labeled pyrimidine derivative through late-stage fluorination reaction using an aryliodonium tosylate as a key intermediate. The in vivo evaluation of this selective PET radioligand in normal rats indicated that our PET radiotracer exhibits a high level of specific binding to 5-HT2C receptors in the rat brain.
E-mail smin92@gmail.com