Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter involved in many physiological and pathological mechanisms through its numerous receptors. Among these, the 5-HT receptor is known to play a key role in multiple brain disorders but remains poorly understood. Positron emission tomography (PET) can contribute to a better understanding of pathophysiological mechanisms regulated by the 5-HT receptor. To develop the first PET radiotracer for the 5-HT receptor, RS-127445, a well-known 5-HT receptor antagonist, was labeled with fluorine-18. [F]RS-127445 was synthesized in a high radiochemical purity and with a good molar activity and radiochemical yield. Preliminary PET scans in rats showed good brain penetration of [F]RS-127445. However, competition experiments and in vitro autoradiography showed high non-specific binding, especially to brain white matter.
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| http://dx.doi.org/10.1016/j.bmcl.2024.129933 | DOI Listing |
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