Serotonin 1A (5-HT1A) receptors are implicated in the pathogenesis of several psychiatric and neurodegenerative disorders motivating the development of suitable radiotracers for in vivo positron emission tomography (PET) neuroimaging. -11C] The gold standard PET imaging agent for this target is [carbonyl WAY-100635, labeled via a technically challenging multi-step reaction that has limited its widespread use. While several antagonist and agonist-based PET radiotracers for 5-HT 1Ar eceptors have been developed, their clinical translation has been hindered by methodological challenges and/or and non-specific binding. As a result, there is continued interest in the development of new and more selective 5-HT1A PET tracers having a relatively easier and reliable radiosynthesis process for routine production and with favorable metabolism to facilitate tracer-kinetic modeling. The purpose of the current study was to develop and characterize a radioligand with suitable characteristics for imaging 5-HT1A receptors in the brain. The current study reports the in vitro characterization and radiosyntheses of three candidate 5 -HT1A receptor antagonists, DF-100 (1), DF-300 (2) and DF-400 (3), to explore their suitability as potential PET radiotracers.

Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers / Narayanaswami, Vidya; Tong, Junchao; Bloomfield Peter, M; Vasdev, Neil; Dahl, Kenneth; Fiorino, Ferdinando; Severino, Beatrice; Sparaco, Rosa; Magli, Elisa; Giordano, Flavia; Bloomfield Peter, M.; Prabhakaran, Jaya; Mann J., John; Vasdev, Neil; Dahl, Kenneth; Kumar J. S., Dileep. - In: EJNMMI RADIOPHARMACY AND CHEMISTRY. - ISSN 2365-421X. - 5:13(2020), pp. 1-17. [10.1186/s41181-020-00096-8]

Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers

Fiorino Ferdinando;Severino Beatrice;Sparaco Rosa;Magli Elisa;Giordano Flavia;
2020

Abstract

Serotonin 1A (5-HT1A) receptors are implicated in the pathogenesis of several psychiatric and neurodegenerative disorders motivating the development of suitable radiotracers for in vivo positron emission tomography (PET) neuroimaging. -11C] The gold standard PET imaging agent for this target is [carbonyl WAY-100635, labeled via a technically challenging multi-step reaction that has limited its widespread use. While several antagonist and agonist-based PET radiotracers for 5-HT 1Ar eceptors have been developed, their clinical translation has been hindered by methodological challenges and/or and non-specific binding. As a result, there is continued interest in the development of new and more selective 5-HT1A PET tracers having a relatively easier and reliable radiosynthesis process for routine production and with favorable metabolism to facilitate tracer-kinetic modeling. The purpose of the current study was to develop and characterize a radioligand with suitable characteristics for imaging 5-HT1A receptors in the brain. The current study reports the in vitro characterization and radiosyntheses of three candidate 5 -HT1A receptor antagonists, DF-100 (1), DF-300 (2) and DF-400 (3), to explore their suitability as potential PET radiotracers.
2020
Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers / Narayanaswami, Vidya; Tong, Junchao; Bloomfield Peter, M; Vasdev, Neil; Dahl, Kenneth; Fiorino, Ferdinando; Severino, Beatrice; Sparaco, Rosa; Magli, Elisa; Giordano, Flavia; Bloomfield Peter, M.; Prabhakaran, Jaya; Mann J., John; Vasdev, Neil; Dahl, Kenneth; Kumar J. S., Dileep. - In: EJNMMI RADIOPHARMACY AND CHEMISTRY. - ISSN 2365-421X. - 5:13(2020), pp. 1-17. [10.1186/s41181-020-00096-8]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/813065
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