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Melatonin is a neurohormone that modulates several physiological functions in mammals through the activation of melatonin receptor type 1 and 2 (MT₁ and MT₂). The melatonergic system is an emerging therapeutic target for new pharmacological interventions in the treatment of sleep and mood disorders; thus, imaging tools to further investigate its role in the brain are highly sought-after. We aimed to develop selective radiotracers for in vivo imaging of both MT₁ and MT₂ by positron emission tomography (PET). We identified four previously reported MT ligands with picomolar affinities to the target based on different scaffolds which were also amenable for radiolabeling with either carbon-11 or fluorine-18. [¹¹C]UCM765, [¹¹C]UCM1014, [¹⁸F]3-fluoroagomelatine ([¹⁸F]3FAGM), and [¹⁸F]fluoroacetamidoagomelatine ([¹⁸F]FAAGM) have been synthesized in high radiochemical purity and evaluated in wild-type rats …