Screening of [F]Florbetazine for Aβ Plaques and a Head-to-Head Comparison Study with [C]Pittsburgh Compound-B ([C]PiB) in Human Subjects.

Positron emission tomography (PET) imaging of amyloid-β (Aβ) has emerged as a crucial strategy for early diagnosis and monitoring of therapeutic advancements targeting Aβ. In our previous first-in-human study, we identified that [F]Florbetazine ([F]), featuring a diaryl-azine scaffold, exhibits higher cortical uptake in Alzheimer's disease (AD) patients compared to healthy controls (HC). Building upon these promising findings, this study aimed to characterize the diagnostic potential of [F] and its dimethylamino-modified tracer [F] and further compare them with the benchmark [C]PiB in the same cohort of AD patients and age-matched HC subjects.

F-labeled somatostatin analogs for somatostatin receptors (SSTRs) targeted PET imaging of neuroendocrine tumors (NETs).

Purpose: A novel F-radiolabeled somatostatin analogue, [AlF]NODA-MPAA-HTA, was synthesized and evaluated for positron emission tomography (PET) imaging of Neuroendocrine tumors (NETs). [AlF]NODA-MPAA-HTA was designed and synthesized by conjugating F nuclide with a modified KE108 peptide, a somatostatin analog with high affinity for all five subtypes of somatostatin receptors (SSTR 1-5), through coupling a bifunctional chelator (NODA) to target somatostatin receptor (SSTR) positive tumors.

Methods: The amino group of KE108 peptide, a SSTRs-targeting pharmacophore, was conjugated with the carboxyl group of NODA by a condensation reaction to obtain the labeling precursor of [AlF]NODA-MPAA-HTA, in which its precursor was obtained through Fmoc solid-phase methods.

Fluorine-18-Labeled Diaryl-azines as Improved β-Amyloid Imaging Tracers: From Bench to First-in-Human Studies.

The deposition of β-amyloid (Aβ) in the brain is a pathologic hallmark of Alzheimer's disease (AD), appearing years before the onset of symptoms, and its detection is incorporated into clinical diagnosis. Here, we have discovered and developed a class of diaryl-azine derivatives for detecting Aβ plaques in the AD brain using PET imaging. After a set of comprehensive preclinical assessments, we screened out a promising Aβ-PET tracer, [F], with a high binding affinity to the Aβ aggregates, significant binding ability with the AD brain sections, and optimal brain pharmacokinetic properties in rodents and non-human primates.

Dynamic Porous Pattern through Controlling Noncovalent Interactions in Polyelectrolyte Film for Sequential and Regional Encapsulation.

Inspired by nature, many functional surfaces have been developed with special structures in biology, chemistry, and materials. Many research studies have been focused on the preparation of surfaces with static structure. Achieving dynamical manipulation of surface structure is desired but still a great challenge.

[High-resolution THz spectra of six biological and pharmaceutical materials].

The temperature dependent vibrational spectra of,three biological and pharmaceutical sets, genistein and biochanin A, clenbuterol hydrochloride and salbutamol, as well as ginseng R2 and R3, in the range of 0.2-4.5 THz (6.