Development of Receptor-Targeted Imaging Agents: Integrated Gallium Complexes and Conjugated Cyclopentadienyl Tricarbonyl Rhenium and Technetium Complexes
Cesati, Richard Raoul, III
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https://hdl.handle.net/2142/84022
Description
Title
Development of Receptor-Targeted Imaging Agents: Integrated Gallium Complexes and Conjugated Cyclopentadienyl Tricarbonyl Rhenium and Technetium Complexes
Author(s)
Cesati, Richard Raoul, III
Issue Date
2000
Doctoral Committee Chair(s)
Katzenellenbogen, John A.
Department of Study
Chemistry
Discipline
Chemistry
Degree Granting Institution
University of Illinois at Urbana-Champaign
Degree Name
Ph.D.
Degree Level
Dissertation
Keyword(s)
Chemistry, Pharmaceutical
Language
eng
Abstract
As the preferred radionuclide for use in Single Photon Emission Computed Tomography (SPECT) imaging is 99mTc, the development of 99mTc-labeled phenyl-tropane analogs with high affinity for the dopamine transporter (DAT) would provide a useful tool for imaging disorders in this transporter system, such as clinical diagnosis of Parkinson's disease. The Direct Double Ligand Transfer (DLT) reaction was developed and utilized in the preparation of several cyclopentadienyltricarbonyl rhenium phenyl-tropanes. N-[4-Oxo-4-cyclopentadienyltricarbonyl rhenium butyl]-2beta-carbomethoxy-[3beta-(4-iodophenyl)] tropane was tested for affinity to the dopamine transporter in rat brain tissue homogenate as a surrogate to the radiolabeled congener. The computed DAT affinity of the rhenium compound was 5.95 +/- 0.93 nM. Regional cerebral uptake and distribution of the technetium-99m congener was evaluated in vivo in mouse brain. At 60 and 90 min after i.v. injection of the technetium compound, the mouse striatum/cerebellum radioactivity ratio was 2.0 and 2.3, and was reduced to unity in presence of beta-CIT at 60 min. The findings show for the first time that a cyclopentadienyltricarbonyltechnetium complex can penetrate mammalian brain tissue and differentially label DAT-rich corpus striatum.
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