PET radiopharmaceuticals for probing enzymes in the brain.
نویسندگان
چکیده
Biologically important processes in normal brain function and brain disease involve the action of various protein-based receptors, ion channels, transporters and enzymes. The ability to interrogate the location, abundance and activity of these entities in vivo using non-invasive molecular imaging can provide unprecedented information about the spatio-temporal dynamics of brain function. Indeed, positron emission tomography (PET) imaging is transforming our understanding of the central nervous system and brain disease. Great emphasis has historically been placed on developing radioligands for the non-invasive detection of neuroreceptors. In contrast, relatively few enzymes have been amenable to examination by PET imaging procedures based upon trapping or accumulation of enzymatic products, because only a subset of enzymes have sufficient catalytic rate to produce measureable accumulation within the practical time-limit of PET recordings. However, high affinity inhibitors are now serving as tracers for enzymes, particularly for measuring the abundance of enzymes mediating intracellular signal transduction in the brain, which offer a rich diversity of potential targets for drug discovery. The purpose of this review is to summarize well-known radiotracers for brain enzymes, and draw attention to recent developments in PET radiotracers for imaging signal transduction pathways in the brain. The review is organized by target class and focuses on structural chemistry of the best-established radiotracers identified in each class.
منابع مشابه
Estimation of fetal absorbed dose from low-dose attenuation-correction CT in PET / CT imaging by using the Body Builder Phantom
One of the methods of studying the physiology and metabolism of important tissues such as the heart, brain and cancer tumors is the use of PET/CT System. A small number of patients are pregnant women who undergo a PET/CT scan due to lack of knowledge about pregnancy or due to dire clinical need. The final dose received by the fetus is based on three factors: the absorbed dose of the fetal tissu...
متن کاملPET Radiopharmaceuticals
PET (positron emission tomography) is a powerful imaging technique that can provide quantitative information on the distribution of positron emitter labeled radiopharmaceuticals (PET radiopharmaceuticals) in the body. Positrons (ß+) are positively charged beta particles. They are emitted when the atom is proton rich. A positron has only a transient existence. After losing all of its kinetic ene...
متن کاملPET radiotracers for molecular imaging in the brain: Past, present and future
Neuroimaging of brain receptors began in the early 1980s. Now, some thirty-five years later, PET imaging is still an expanding field of preclinical and clinical investigations. In addition to improvements in PET cameras and image analysis, the availability of suitable radiotracers is a crucial factor leading this expansion. Radiotracers have been developed to visualize and quantify a growing nu...
متن کاملMolecular Targets for PET Imaging of Activated Microglia: The Current Situation and Future Expectations
Microglia, as cellular mediators of neuroinflammation, are implicated in the pathogenesis of a wide range of neurodegenerative diseases. Positron emission tomography (PET) imaging of microglia has matured over the last 20 years, through the development of radiopharmaceuticals targeting several molecular biomarkers of microglial activation and, among these, mainly the translocator protein-18 kDa...
متن کاملAn overview on Ga-68 radiopharmaceuticals for positron emission tomography applications
Gallium-68 a positron emitter radionuclide, with great impact on the nuclear medicine, has been widely used in positron emission tomography (PET) diagnosis of various malignancies in humans during more recent years especially in neuroendocrine tumors (NETs). The vast number of 68Ge/68Ga related generator productions, targeting molecule design (proteins, antibody fragments,...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- American journal of nuclear medicine and molecular imaging
دوره 3 3 شماره
صفحات -
تاریخ انتشار 2013