1419268-86-2Relevant articles and documents
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [125I]Flip-IDAM, (2-((2-((dimethylamino) methyl)-4-iodophenyl)thio)phenyl)methanol
Zheng, Pinguan,Lieberman, Brian P.,Ploessl, Karl,Lemoine, Laetitia,Miller, Sara,Kung, Hank F.
supporting information, p. 869 - 872 (2013/03/13)
New ligands for in vivo brain imaging of serotonin transporter (SERT) with single photon emission tomography (SPECT) were prepared and evaluated. An efficient synthesis and radiolabeling of a biphenylthiol, FLIP-IDAM, 4, was accomplished. The affinity of FLIP-IDAM was evaluated by an in vitro inhibitory binding assay using [125I]-IDAM as radioligand in rat brain tissue homogenates (Ki = 0.03 nM). New [125I]Flip-IDAM exhibited excellent binding affinity to SERT binding sites with a high hypothalamus to cerebellum ratio of 4 at 30 min post iv injection. The faster in vivo kinetics for brain uptake and a rapid washout from non-specific regions provide excellent signal to noise ratio. This new agent, when labeled with 123I, may be a useful imaging agent for mapping SERT binding sites in the human brain.