Novel styrylpyridines as probes for SPECT imaging of amyloid plaques
| Autor: | Wenchao Qu, Tyler E. Benedum, Hank F. Kung, Catherine Hou, Mei-Ping Kung |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Male
Pathology medicine.medical_specialty Amyloid Pyridines Plaque Amyloid Single-photon emission computed tomography Binding Competitive Cell Line Styrenes Iodine Radioisotopes Mice Radioligand Assay Structure-Activity Relationship In vivo Alzheimer Disease Spect imaging Drug Discovery medicine Animals Humans Tissue Distribution Tomography Emission-Computed Single-Photon Mice Inbred ICR Amyloid beta-Peptides medicine.diagnostic_test Chemistry Brain Human brain medicine.disease Ligand (biochemistry) In vitro medicine.anatomical_structure Molecular Medicine Autoradiography Alzheimer's disease Radiopharmaceuticals |
| Zdroj: | Journal of medicinal chemistry. 50(9) |
| ISSN: | 0022-2623 |
| Popis: | We report a series of radioiodinated styrylpyridines as single photon emission computed tomography probes for imaging Abeta plaques in the brain of patients with Alzheimer's disease (AD). In vitro binding showed that all of the styrylpyridines displayed very good binding affinities in postmortem AD brain homogenates (Ki = 3.6 to 15.5 nM). No-carrier-added samples of 13a, 13b, 16a, 16b, and 16e (radioiodinated with 125I) were successfully prepared. The in vivo biodistribution in normal mice, at 2 min after injection, showed excellent initial brain penetrations (4.03, 6.22, 5.43, and 8.04% dose/g for [125I]13a, 13b, 16a, and 16b, respectively). Furthermore, in vitro autoradiography of AD brain sections showed that the high binding signal was specifically due to the presence of Abeta plaques. Taken together, these results strongly suggest that these styrylpyridines are useful for imaging Abeta plaques in the living human brain. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|