A peptide-based near-infrared fluorescence probe for dynamic monitoring senile plaques in Alzheimer's disease mouse model.

In vivo monitoring neuropathological changes in Alzheimer's disease (AD) animal model is critical for drug development. Here, by integrating blood-brain barrier penetrable peptide, we have developed a peptide probe which based on angiopep-2. Angiopep-based probe exhibited high binding affinity to Aβ aggregates and labeled senile plaques in vivo.

Synthesis and biological evaluation of curcumin analogs as β-amyloid imaging agents.

Aim: Detection of β-amyloid (Aβ) plaques in the brain is a very promising biomarker approach for early diagnosis of Alzheimer's disease (AD).

Materials & Methods: A series of curcumin analogs (1,5-diphenyl-1,4-pentadien-3-one derivatives) were synthesized and evaluated. Specific binding to Aβ plaques was demonstrated in vitro using postmortem AD homogenates, and the fluorescent staining and autoradiography in vitro of postmortem AD brain sections were performed.

6-Methoxy-indanone derivatives as potential probes for β-amyloid plaques in Alzheimer's disease.

A series of 6-methoxy indanone derivatives was synthesized and evaluated as potential probes for β-amyloid plaque imaging in Alzheimer's disease (AD). Two derivatives (5d and 5k) displayed significant binding abilities in fluorescent staining experiments using the brain sections of AD patients. Two derivatives showed high binding affinities to β-amyloid aggregates (5j, K = 5.

Homoisoflavonoids as potential imaging agents for β-amyloid plaques in Alzheimer's disease.

A series of homoisoflavonoids [(E)-3-benzylidenechroman-4-ones, 3a-l] as novel potential diagnostic imaging agents targeting β-amyloid (Aβ) plaques in Alzheimer's disease (AD) were synthesized and evaluated. In vitro binding studies using Aβ₁₋₄₀ aggregates with [(125)I]IMPY as the reference ligand showed that these compounds demonstrated high to low binding affinities at the K(i) values ranged from 9.10 to 432.

Novel indanone derivatives as potential imaging probes for β-amyloid plaques in the brain.

Molecular imaging probes to detect senile plaques (SPs) might help the early diagnosis of Alzheimer's disease (AD). In this study, a novel series of indanone derivatives were synthesized and characterized. In in vitro binding studies, compound 2e exhibited a K(i) value of 16 nM with a human AD brain homogenate.