Researchers have developed a new imaging agent that could help guide and assess treatments for people with various neurological diseases, including Alzheimer's, Parkinson's, and multiple sclerosis. The agent, which is used in positron emission tomography (PET) scans, targets receptors in nerve cells in the brain that are involved in learning and memory. The study is featured in the April issue of The Journal of Nuclear Medicine.
Swiss and German scientists developed the new PET radioligand, 11C-Me-NB1, for imaging GluN1/GluN2B-containing N-methyl-D-aspartate (NMDA) receptors (a class of glutamate receptor) in nerve cells.
When NMDA receptors are activated, there is an increase of calcium (Ca2+) in the cells, but Ca2+ levels that are too high can cause cell death. Medications that block NMDA receptors are therefore used for the treatment of a wide range of neurological conditions from depression, neuropathic pain and schizophrenia to ischemic stroke and diseases causing dementia.
"The significance of the work lies in the fact that we have for the first time developed a useful PET radioligand that can be applied to image the GluN2B receptor subunit of the NMDA receptor complex in humans," explains Simon M. Ametamey, PhD, of the Institute of Pharmaceutical Sciences, ETH Zurich, in Switzerland.
"The availability of such a PET radioligand would not only help to better understand the role of NMDA receptors in the pathophysiology of the many brain diseases in which the NMDA receptor is implicated, but it would also help to select appropriate doses of clinically relevant GluN2B receptor candidate drugs. Administering the right dose of the drugs to patients will help minimize side-effects and lead to improvement in the efficacy of the drugs."
For the study, 11C-Me-NB1 was used in live rats to investigate the dose and effectiveness of eliprodil, a drug that blocks the NMDA GluN2B receptor. PET scans with the new radioligand successfully showed that the receptors are fully occupied at neuroprotective doses of eliprodil. The new radioligand also provided imaging of receptor crosstalk between Sigma-1 receptors, which modulate calcium signaling, and GluN2B-containing NMDA receptors.
Ametamey points out, "These results mean that a new radiopharmaceutical tool is now available for studying brain disorders such as Alzheimer`s disease, Parkinson`s disease and multiple sclerosis, among others. It joins the list of existing PET radiopharmaceuticals used in imaging studies to investigate and understand underlying causes of these brain disorders." He adds, "Furthermore, future imaging studies using this new radioligand would throw more light on the involvement of NMDA receptors, specifically the GluN2B receptors, in normal physiological processes such as learning and memory, as well as accelerate the development of GluN2B candidate drugs currently under development."
Authors of "Evaluation of 11C-Me-NB1 as a potential PET radioligand for measuring GluN2B?containing NMDA receptors, drug occupancy and receptor crosstalk" include Stefanie D. Krämer, Thomas Betzel, Ahmed Haider, Adrienne Herde Müller, Anna K. Boninsegni, Claudia Keller, Roger Schibli and Simon M. Ametamey, Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland; Linjing Mu, University Hospital Zurich, Zurich, Switzerland; and Marina Szermerski and Bernhard Wünsch, University of Munster, Munster, Germany.
This study was financially supported by the Swiss National Science Foundation (Grant Number 160403).
Please visit the SNMMI Media Center to view the PDF of the study, including images, and more information about molecular imaging and personalized medicine. To schedule an interview with the researchers, please contact Laurie Callahan at (703) 652-6773 or email@example.com. Current and past issues of The Journal of Nuclear Medicine can be found online at http://jnm.
ABOUT THE SOCIETY OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
The Society of Nuclear Medicine and Molecular Imaging (SNMMI) is an international scientific and medical organization dedicated to advancing nuclear medicine and molecular imaging, vital elements of precision medicine that allow diagnosis and treatment to be tailored to individual patients in order to achieve the best possible outcomes.
SNMMI's more than 15,000 members set the standard for molecular imaging and nuclear medicine practice by creating guidelines, sharing information through journals and meetings and leading advocacy on key issues that affect molecular imaging and therapy research and practice. For more information, visit http://www.
Laurie Callahan | EurekAlert!
Smartphone cameras can speed up urinary tract infection diagnosis
08.01.2020 | University of Bath
Livestream from the Digestive System: Magnet-Guided Camera Capsules for More Pleasant Gastroscopies
06.01.2020 | Fraunhofer-Institut für Zuverlässigkeit und Mikrointegration IZM
For years, a new synthesis method has been developed at TU Wien (Vienna) to unlock the secrets of "strange metals". Now a breakthrough has been achieved. The results have been published in "Science".
Superconductors allow electrical current to flow without any resistance - but only below a certain critical temperature. Many materials have to be cooled down...
KIT researchers develop novel composites of DNA, silica particles, and carbon nanotubes -- Properties can be tailored to various applications
Using DNA, smallest silica particles, and carbon nanotubes, researchers of Karlsruhe Institute of Technology (KIT) developed novel programmable materials....
Styrofoam or copper - both materials have very different properties with regard to their ability to conduct heat. Scientists at the Max Planck Institute for Polymer Research (MPI-P) in Mainz and the University of Bayreuth have now jointly developed and characterized a novel, extremely thin and transparent material that has different thermal conduction properties depending on the direction. While it can conduct heat extremely well in one direction, it shows good thermal insulation in the other direction.
Thermal insulation and thermal conduction play a crucial role in our everyday lives - from computer processors, where it is important to dissipate heat as...
In order to advance the transfer of research developments from the field of quantum sensor technology into industrial applications, an application laboratory is being established at Fraunhofer IAF. This will enable interested companies and especially regional SMEs and start-ups to evaluate the innovation potential of quantum sensors for their specific requirements. Both the state of Baden-Württemberg and the Fraunhofer-Gesellschaft are supporting the four-year project with one million euros each.
The application laboratory is being set up as part of the Fraunhofer lighthouse project »QMag«, short for quantum magnetometry. In this project, researchers...
Microtubules, filamentous structures within the cell, are required for many important processes, including cell division and intracellular transport. A...
16.01.2020 | Event News
15.01.2020 | Event News
07.01.2020 | Event News
21.01.2020 | Materials Sciences
21.01.2020 | Health and Medicine
21.01.2020 | Life Sciences