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ID: ALA1138413

Journal: Bioorg Med Chem Lett

Title: Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.

Authors: Tamagnan GD, Brenner E, Alagille D, Staley JK, Haile C, Koren A, Early M, Baldwin RM, Tarazi FI, Baldessarini RJ, Jarkas N, Goodman MM, Seibyl JP.

Abstract: A series of reboxetine analogs was synthesized and evaluated for in vitro binding as racemic mixtures. The best candidate (INER) was synthesized as the optically pure (S,S) enantiomer, labeled with iodine-123 and its in vivo binding determined by SPECT imaging in baboons. The in vivo specificity, selectivity, and kinetics of [123I]INER make it a promising agent for imaging NET in vivo by noninvasive SPECT imaging.

CiteXplore: 17095215

DOI: 10.1016/j.bmcl.2006.10.018