Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2024

[18F]RS-127445 radiosynthesis and evaluation as a 5-HT2B receptor PET radiotracer in rat brain

Résumé

Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter involved in many physiological and pathological mechanisms through its numerous receptors. Among these, the 5-HT2B 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-HT2B receptor. To develop the first PET radiotracer for the 5-HT2B receptor, RS-127445, a well-known 5-HT2B receptor antagonist, was labeled with fluorine-18. [18F]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 [18F]RS-127445. However, competition experiments and in vitro autoradiography showed high non-specific binding, especially to brain white matter.

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Dates et versions

hal-04794525 , version 1 (23-01-2025)

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Violette Richin, Caroline Bouillot, Sandrine Bouvard, Pierre Courault, Sophie Lancelot, et al.. [18F]RS-127445 radiosynthesis and evaluation as a 5-HT2B receptor PET radiotracer in rat brain. Bioorganic and Medicinal Chemistry Letters, 2024, 112, pp.129933. ⟨10.1016/j.bmcl.2024.129933⟩. ⟨hal-04794525⟩
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