AI Article Synopsis
Article Abstract
Translocator protein 18 kDa (TSPO) is a biomarker of neuroinflammation. [C]ER176 robustly quantifies TSPO in the human brain with positron emission tomography (PET), irrespective of subject genotype. We aimed to develop an ER176 analog with potential for labeling with longer-lived fluorine-18 ( = 109.8 min). New fluoro and trifluoromethyl analogs of ER176 were prepared through a concise synthetic strategy. These ligands showed high TSPO affinity and low human genotype sensitivity. Each ligand was initially labeled by a generic C-methylation procedure, thereby enabling speedy screening in mice. Each radioligand was rapidly taken up and well retained in the mouse brain at baseline after intravenous injection. Preblocking of TSPO showed that high proportions of brain uptake were specifically bound to TSPO at baseline. Overall, the 3-fluoro analog of [C]ER176 ([C]) displayed the most promising imaging properties. Therefore, a method was developed to label with [F]fluoride ion. [F] gave similarly promising PET imaging results and deserves evaluation in higher species.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8817670 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.1c01562 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Effect of D-amino acid metabolic enzyme deficiency on cancer development-diffuse large B-cell lymphoma onset and gene expression analyses in DASPO-knockout mice.
Amino Acids
December 2024
Department of Nephrology and Rheumatology, Kanazawa University, 13-1 Takara-Machi, Kanazawa, 920-8641, Japan.
The relationship between D-AA metabolic enzymes and cancer development remains unclear. We aimed to investigate this relationship using mice deficient in D-AA-related metabolic enzymes. We examined mice lacking these enzymes for approximately 900 days and the effects of altered D-AA metabolism on cancer development based on lifespan, pathological findings, and gene expression.
View Article and Find Full Text PDFPhotoacoustic and fluorescence dual-modality imaging of cerebral biomarkers in Alzheimer's disease rodent model.
J Biomed Opt
December 2024
University of Michigan, Department of Biomedical Engineering, Ann Arbor, Michigan, United States.
Significance: Alzheimer's disease (AD) is a predominant form of dementia that can lead to a decline in the quality of life and mortality. The understanding of the pathological changes requires monitoring of multiple cerebral biomarkers simultaneously with high resolution. Photoacoustic microscopy resolves single capillaries, allowing investigations into the most affected types of vessels.
View Article and Find Full Text PDFExosomes from IH- Induced bEnd3 Cells Promote OSA Cognitive Impairment via miR-20a-5p/MFN2 Mediated Pyroptosis of HT22 Cells.
Nat Sci Sleep
December 2024
Department of Pulmonary and Critical Care Medicine, The Second Xiangya Hospital, Central South University, Changsha, Hunan, 410011, People's Republic of China.
Background: OSA can cause cognitive impairment (CI). The aim of this study was to investigate whether miR-20a-5p in exosomes derived from bEnd3 cells with IH mediates intercellular crosstalk and induces CI through hippocampal neuronal cell pyroptosis.
Materials And Methods: BEnd3-derived exosomes were isolated from the normal oxygen control group (NC-EXOS) and IH group (IH-EXOS).
Macrophage Notch1 signaling modulates regulatory T cells via the TGFB axis in early MASLD.
JHEP Rep
January 2025
Department of Pharmacology, Wuhan University TaiKang Medical School (School of Basic Medical Sciences), Wuhan 430071, China.
Background & Aims: Hepatic immune imbalance is crucial for driving metabolic dysfunction-associated steatotic liver disease (MASLD) progression. However, the role of hepatic regulatory T cells (Tregs) in MASLD initiation and the mechanisms responsible for their change are not completely understood.
Methods: A mouse model subjected to a short-term high-fat diet (HFD) to mimic early steatosis, along with liver biopsy samples from patients with simple steatosis, and macrophage-specific Notch1-knockout mice (Notch1), were used to investigate the role of Tregs in early MASLD and the effect of hepatic macrophage Notch1 signaling on Treg frequency.
Spatially Preorganized Hybridization Chain Reaction for the Prompt Diagnosis of Inflammation.
Angew Chem Int Ed Engl
December 2024
Nanjing University, Department of Biomedical Engineering, CHINA.
Biological systems utilize precise spatial organization to facilitate and regulate information transmission within signaling networks. Inspired by this, artificial scaffolds that enable delicate spatial arrangements are desirable to increase the local concentration of reactants, expedite specific interactions, and minimize undesired interference. In this study, we presented an integrated biosensing nanodevice, termed TRI-HCR, in which hybridization chain reaction (HCR) probes were precisely organized on a triangular DNA origami nanostructure (TRI) with finely-tuned distance, quantity, and pattern.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!