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Leung K1.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2011 Aug 10 [updated 2011 Nov 03].

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National Center for Biotechnology Information, NLM, NIH


Dopamine, a neurotransmitter, plays an important role in the mediation of movement, cognition, and emotion. Parkinson’s disease (PD) is associated with a loss of dopamine-containing neurons in the striatum, resulting in a loss of dopamine transporter (DAT) in the presynaptic nerve terminals (1, 2). Reduction of DAT density is inversely correlated with the severity of motor dysfunction in PD patients. Several (-)-cocaine analogs were developed for the evaluation of DAT density in neurons of PD patients. Radiolabeled 2β-carboxymethoxy-3β-(4-iodophenyl)tropane (β-CIT) and N-(3-fluoropropyl)-2β-carbomethoxy-3β-(4-iodophenyl)nortropane (FP-CIT) have been used for brain imaging (3-6). Because of the short physical half-life of 11C-labeled analogs, equilibrium conditions are difficult to achieve in positron emission tomography (PET) measurements. [123I]β-CIT was studied in single-photon emission computed tomography (SPECT) and showed slow tracer uptake kinetics (7, 8). A tropane derivative, [11C]-(E)-N-(4-fluorobut-2-enyl)-2β-carbomethoxy-3β-(4'-tolyl)nortropane ([11C]LBT-999), was evaluated as a radioligand for studies of DAT with PET imaging (9-11). N-4-[18F]Fluorobut-2-yn-1-yl-2β-carbomethoxy-3β-phenyltropane ([18F]PR04.MZ) was developed through the use of a conformational restriction approach based on (-)-cocaine (12). PR04.MZ exhibited a 100-fold higher potency than (-)-cocaine in inhibition of human DAT and better selectivity over the human noradrenalin transporter (hNET) and human serotonin transporter (hSERT). [18F]PR04.MZ has been evaluated as a radioligand for studies of DAT with PET imaging.

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