Coloquio de Medicina Nuclear:
Radiofármacos para neuroimágenes con PET
Dr. Vasko Kramer, Positronpharma S.A.
“Ligands for pre- and postsynaptic imaging of the dopaminergic system in
neurodegenerative disorders by PET”
Dr. Matthias Herth, Center for Integrated Molecular Brain Imaging,
Rigshospitalet and University of Copenhagen
“Neuo-PET ligand development: From medicinal chemistry to human PET
- Fecha: 14 de Febrero 2013 de 18:00 a 19:30
- Lugar: Auditorio de la Fundación Arturo Lopez Perez, Rancagua 878, Providencia, Santiago
Dr. Matthias Herth
Center for Integrated Molecular Brain Imaging, Rigshospitalet and University of Copenhagen, and Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copen
Systematic Development Approaches for Novel PET Tracers 1) A case study for the development of a 5-HT7 brain receptor ligand 2) Design of in vivo click imaging agents
1) A successful in vivo imaging probe for neuroreceptors possesses a range of properties including high selectivity for the target of interest, the ability to reach the target site, low nonspecific binding, suitable affinity such that a large enough specific-to nonspecific signal exists, suitably reversible kinetics to facilitate quantitative analysis, and the ability to be radiolabeled. Given these numerous and sometimes conflicting characteristics, it is not surprising that the discovery and development process is challenging. To date, the process usually concentrates on screening compounds according to lipophilicity, affinity, selectivity and labeling feasibility. The weakness of these approaches is that only some of the characteristics required are considered, with little deliberation given to the prediction of nonspecific binding and optimal kinetics. In this talk, I want to present the development design which we have applied for a 5-HT7 tracer and which strategies we want to implement in the future.
2) Developing new approaches for diagnosing and treating cancer as well as neurodegenerative brain diseases currently remain major tasks for our society and current healthcare systems. Promising approaches to develop efficient therapies or to explore molecular basis of various diseases are hampered by missing long-term in vivo clinical imaging techniques. PET (Positron Emission Tomography) is an appropriate tool to image in vivo long-term drug interactions. But current methods apply long-lived radionuclides and are thus inadequate for clinical long-term PET imaging. Major drawbacks are high absorbed radiation doses and restricted patient mobility. In this talk, I want to show possibilities to circumvent this problem using in vivo click imaging strategies. A short state of the art review and an overview of my future research plan will be presented.