Characterization of 4-[18F]-ADAM as an imaging agent for SERT in non-human primate brain using PET: a dynamic study

Characterization and Reliability of [18F]2FNQ1P in Cynomolgus Monkeys as a PET Radiotracer for Serotonin 5-HT6 Receptors

“…Compared to similar reproducibility studies published for other PET tracers of the serotoninergic system in primates (Chen et al, 2012; Tavares et al, 2014), the reproducibility parameters of [ 18 F]2FNQ1P binding potential showed more satisfactory results. In consequence, the ability to detect changes in 5-HT 6 R availability or occupancy in in vivo studies, would be more sensitive with [ 18 F]2FNQ1P, giving a supplemental chance of elucidating functional and dysfunctional serotonin transmission in the brain and facilitating the development of therapeutic drugs targeting 5-HT 6 Rs.…”

Incongruent Reduction of Serotonin Transporter Associated with Suicide Attempts in Patients with Major Depressive Disorder: A Positron Emission Tomography Study with 4-[18F]-ADAM

“…To reduce the confounding effects of SERT binding in the cerebellum, the white matter and vermis were excluded, and only the posterior half of the cerebellar cortex was delineated. The BP of 4-[ 18 F]-ADAM was quantified using a previously-described ratio method by comparing specifically-bound radioligands to nondisplaceable radioligands in brain tissue (BP ND ) at equilibrium ( Shiue et al, 2003 ; Chen et al, 2012 ; Huang et al, 2013 ). Because the uptake of 4-[ 18 F]-ADAM has been reported to reach equilibrium about 120–140min after its injection in human subjects ( Huang et al, 2013 ), we selected the 120min frames for the equilibrium ratio method in our modeling.…”

Deuterium‐substituted 2‐(2′‐((dimethylamino)methyl)‐4′‐[18F](fluoropropoxy)phenylthio)benzenamine as a serotonin transporter imaging agent

“…The 18 F labeling reaction was accomplished by using a 1step labeling reaction (Scheme 2). The labeling reaction was performed by reacting precursor, 7, with activated 18 F fluoride (in the presence of Kryptofix 222 and potassium carbonate) in acetonitrile at 80°C for 15 minutes, which gave [ 18 F]1. The crude mixture was purified by HPLC.…”

“…3 Positron emission tomography (PET) imaging for SERT binding sites in the brain with [ 11 C]DASB (T 1/2 = 20 min) ( Figure 2) has been reported, and its clinical application is well reported in the literature. [4][5][6][7] A suitably 18 F-labeled SERT imaging agent with its longer physical half-life (T 1/2 = 110 min) is more convenient to manufacture and distribute for probing pathophysiological and therapeutic mechanisms in various psychological diseases. 8 A number of SERT ligands for in vivo imaging ( Figure 2) have been developed.…”

“…8 A number of SERT ligands for in vivo imaging ( Figure 2) have been developed. [9][10][11][12][13][14][15][16][17][18][19][20][21] Biphenyl sulfide derivatives showed promising results as in vivo SERT imaging agents ( Figure 2). 22 This biphenyl sulfide series of imaging agents display one unique advantage over other series, because they are highly selective towards SERT binding and have low affinity to dopamine transporter and norepinephrine transporters.…”