Clinical agents radiopharmaceuticals

The main radiopharmaceuticals labelled with fluorine-18, routinely prepared ([2-i F] fluorodeoxyglucose [ F]FDG [26-28], [i F]fluoro-L-DOPA [29], [i F]altanserin [30, 31], [ F]setoperone [32]) are presented with their uses in Table 2. For comparison, the most common tracers labelled with carbon-11 (methionine [33], palmitic acid [34], flumazenil (RO 15.1788) [35], PK 11195 [36], raclopride [37], deprenyl [38], Way-100635 [39], McN-5652Z [40], CGP 12177 [41]) are shown in Table 3. By far, [ F]FDG is the most widely studied, particularly in oncology for the diagnosis of tumours, detection of sub-clinical diseases, assessment of therapy responses, and detection of recurrence. F-Steroids [42], F-proteins or peptides, or F-labelled tissue specific agents have also been synthesized for the detection and monitoring of various malignancies [43]. 

Brain Agents. Tc radiopharmaceuticals that penetrate the blood brain barrier (BBB) are generally small, neutral, and lipophilic. Moreover, to be useful for imaging, the molecules must possess some mechanism of retention. Clinical brain imaging studies with 9 Tc, aimed at detection of regional cerebral blood flow changes, are performed with D, E-99 Tc-HMPAO, Ceretec , or E, E-99 Tc-ECD, Neurolite (Figure 2). Both are small, neutral molecules that cross the BBB and are retained in the brain. 

Technetium ( Tcj Bicisate Injection. A sterile colorless solution of bicisate is complexed with Tc-99m pertech-neuite after reduction with a stannous salt. The precise structure of the technetium complex is fN,N -ethylene-di-L-cy.steinato(3-) oxo "Tc]technetium(V) diethyl ester. This radiopharmaceutical is a neutral and lipophilic complex that crosses the blotxl-brain barrier and is selectively retained in the brain. Therefore, this radiotracer is used as a brain-perfusion imaging agent. After intravenous injection of 20 mCi (740 MBq) of Tc-99m bicisate, about 5% of the injected dose is localized within the brain cells 5 minutes after injection and demonstrates rapid renal excretion (74% in 24 hours). This radiotracer is used clinically to evaluate dementia, stroke, lack of brain perfusion ("brain death"), cerebral vascular reserve, or risk of stroke (acetazolamide challenge. study) and to localize a seizure focus for surgical removal. 

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