A new imaging agent has been developed by scientists that can assist to direct and evaluate therapies for individuals with numerous neurological diseases, comprising Parkinson’s, multiple sclerosis, and Alzheimer’s. The agent—that is utilized in PET (positron emission tomography) scans—aims receptors in brain nerve cells that are concerned with memory and learning.
11C-Me-NB1, the new PET radioligand, is developed by the German and Swiss researchers to map GluN1/GluN2B-enclosing NMDA (N-methyl-D-aspartate) receptors in nerve cells. There is a rise in ca2+ (calcium) in the cell when the NMDA receptors are triggered; however, very high levels of Ca2+ can result in cell death. Thus, drugs that chunk NMDA receptors are utilized for the treating a broad array of neurological conditions from neuropathic pain, schizophrenia, and depression to diseases resulting in dementia and ischemic stroke.
Simon M. Ametamey from the Institute of Pharmaceutical Sciences, explains, “The importance of the effort lies in the reality that we’ve for the foremost instance designed a valuable PET radioligand that could be used to map the NMDA receptor complex’s GluN2B receptor subunit in humans.”
“The accessibility of such a PET radioligand will not only assist to improve comprehending the NMDA receptors’ role in the pathophysiology of several brain diseases, wherein the NMDA receptor is involved, but it will also assist to choose correct dosages of clinically pertinent GluN2B receptor candidate medications. Giving the appropriate drug dose to patients will assist to reduce the side-effects and result in improvement in the drugs’ efficacy.”
For the research, 11C-Me-NB1 was utilized in live rats to examine the effectiveness and dose of eliprodil, a medication that chunks the NMDA GluN2B receptor. The results of PET scans with the novel agent successfully demonstrated that the receptors are completely taken at eliprodil’s neuroprotective doses. The new radioligand also offered mapping of receptor crosstalk between GluN2B-enclosing NMDA receptors and Sigma-1 receptors—that regulate calcium signaling.