Current Topics in Medicinal Chemistry - Volume 13, Issue 8, 2013

18F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given 18F-labeled amino acid depends largely upon its mechanism of transport. The system L amino acid transport system has been a major focus of trac Read More

In recent years, two different methods have been developed to image cell proliferation with the functional imaging technique, Positron emission Tomography (PET), proliferation rate and proliferative status. Proliferation rate is a measure of the tumor doubling time and uses radiolabeled analogs of the DNA precursor thymidine. This approach measures the activity of the enzyme thymidine kinase 1 (TK1) and provides a pu Read More

Alzheimer's disease (AD), the most common form of dementia, is a progressive and fatal neurodegenerative disorder. The neuropathological hallmarks of AD generally revealed on postmortem brain tissue are the extracellular neuritic plaque deposits and intracellular neurofibrillary tangles. Significant evidence supports the pivotal role of β-amyloid peptides in the pathogenesis of AD. Therefore, The ability to image β Read More

The development of tropane-derivatives as cocaine-addiction therapeutics identified numerous compounds with affinities for the dopamine, serotonin, and norepinephrine transporters. Many of these compounds were then adapted for use as imaging radiotracers. Incorporation of fluorine into the molecule often improved the physiochemical properties of the compound and also provided a position for radiolabeling Read More

Diaryl sulfides also known as diphenyl sulfides, phenylthiobenzylamines, and biphenylthiols are a class of compounds with phenylthiophenyl scaffold that have been validated as biomarkers to label the brain serotonin transporter (SERT), in vivo. The development of those synthetic and non-natural compounds started more than a decade ago when the observation that 5-chloro-((2-((dimethylamino)methyl)phenyl)thio)benzene-meth Read More

2-Deoxy-2-[18F]fluoro-D-glucose (2-18FDG) has represented radiofluorinated carbohydrates as the most successful tracer for positron emission tomography (PET). 2-18FDG uptake depends on glucose metabolism, which is related to a disease progression. 2-18FDG has been widely used in oncology, neurology, cardiology, infectious diseases, and inflammation, to complement anatomical modalities such as CT and MRI. Follo Read More

Prostate cancer (PCa) is the second leading cause of cancer-related death in American men. Positron emission tomography/computed tomography (PET/CT) with emerging radiopharmaceuticals promises accurate staging of primary disease, restaging of recurrent disease, detection of metastatic lesions and, ultimately, for predicting the aggressiveness of disease. Prostate-specific membrane antigen (PSMA) is a well-ch Read More