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Development of a novel radioiodinated compound for amyloid and tau deposition imaging in Alzheimer's disease and tauopathy mouse models.
Neuroimage
December 2024
Department of Radiopharmacy and Molecular Imaging, Minhang Hospital & School of Pharmacy, Fudan University, Shanghai, China; Department of Functional Brain Imaging Research, China; Department of Clinical and Experimental Neuroimaging, Centre for Development of Advanced Medicine for Dementia, National Centre for Geriatrics and Gerontology, Obu, Japan; Key Laboratory of Smart Drug Delivery, Fudan University, Ministry of Education, Shanghai, China; Institute for Small-Molecule Drug Discovery & Development, Quzhou Fudan Institute, Quzhou, China. Electronic address:
Article Synopsis
- - The study focused on a new compound called AD-DRK (I-AD-DRK) that can non-invasively identify amyloid-β and tau deposits in the brain, which are critical for diagnosing Alzheimer's disease and related disorders.
- - Researchers conducted tests using this compound in both postmortem human brains and mouse models with amyloid and tau accumulation, demonstrating its effective binding and visualization capabilities in the brain regions associated with these proteins.
- - The results showed that I-AD-DRK has strong potential as a SPECT imaging agent, offering high-contrast imaging of amyloid and tau, which could significantly help in early diagnosis and treatment of Alzheimer's disease and other tauopathies.
Discovery of F Labeled AZD5213 Derivatives as Novel Positron Emission Tomography (PET) Radioligands Targeting Histamine Subtype-3 Receptor.
Chembiochem
September 2024
Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, Atlanta, GA, 30322, USA.
The histamine subtype 3 (H) receptor is an important drug target in the central nervous system (CNS), and PET imaging offers a promising technique for the noninvasive evaluation of CNS disease related to the H receptor. In this study, we synthesized and evaluated the binding effects of [F]H3-2404 and [F]H3-2405 by modifying the structure of AZD5213, a selective H antagonist. These two radioligands were prepared in high radiochemical yields and displayed stability in serum.
View Article and Find Full Text PDFAssessment of Radiolabelled Derivatives of R954 for Detection of Bradykinin B1 Receptor in Cancer Cells: Studies on Glioblastoma Xenografts in Mice.
Pharmaceuticals (Basel)
July 2024
Laboratory of Physical Chemistry, Showa Pharmaceutical University, Tokyo 194-8543, Japan.
Bradykinin B1 receptor (B1R) has garnered attention as a cancer therapeutic and diagnostic target. Several reports on radiolabelled derivatives of B1R antagonists have shown favourable properties as imaging agents in cells highly expressing hB1R following transfection. In the present study, we assessed whether radiolabelled probes can detect B1R endogenously expressed in cancer cells.
View Article and Find Full Text PDFBiodistribution of Drug/ADA Complexes: The Impact of Immune Complex Formation on Antibody Distribution.
AAPS J
March 2024
Roche Pharma Research and Early Development, Pharmaceutical Sciences, Roche Innovation Center Munich, Roche Diagnostics GmbH, Nonnenwald 2, DE-82377, Penzberg, Germany.
The clinical use of therapeutic monoclonal antibodies (mAbs) for the treatment of cancer, inflammation, and other indications has been successfully established. A critical aspect of drug-antibody pharmacokinetics is immunogenicity, which triggers an immune response via an anti-drug antibody (ADA) and forms drug/ADA immune complexes (ICs). As a consequence, there may be a reduced efficacy upon neutralization by ADA or an accelerated drug clearance.
View Article and Find Full Text PDFQuantitative Analysis of S1PR1 Expression in the Postmortem Multiple Sclerosis Central Nervous System.
ACS Chem Neurosci
November 2023
Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, United States.
Article Synopsis
- - Multiple sclerosis (MS) is an immune-related disease that leads to damage in the central nervous system (CNS), predominantly affecting myelin and causing inflammation.
- - This study investigated the role of the S1PR1 receptor in MS by measuring its expression in brain tissues from MS patients and comparing it to healthy controls, revealing significantly higher levels in MS lesions.
- - The research suggests that targeting S1PR1 could be beneficial for imaging and understanding MS pathology, as the S1PR1-specific radioligand showed increased binding in areas affected by the disease.
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