1537191-14-2

Upstream product

• 14099-01-5 rhenium(I) pentacarbonyl chloride 
• 1537191-04-0 4-(5-(5-(bis(pyridin-2-ylmethyl)amino)pentyloxy)benzo(d)thiazol-2-yl)-N,N-dimethylbenzenamine 
• 111-24-0 1,5-dibromo-pentane 
• 1537191-01-7 4-(5-(5-bromopentyloxy)benzo[d]thiazol-2-yl)-N,N-dimethylbenzenamine 

Downstream Products

• 1537191-23-3 C₃₅H₃₅N₅O₄S⁽⁹⁹⁾Tc⁽¹⁺⁾*Cl^(1-) 

Relevant academic research and scientific papers

Plaque A β having affinity with the 2-aryl benzo thiazole compound, preparation method and application thereof

The invention provides a 2-aryl benzothiazole compound with high affinity with A(beta) plaque and a preparation method and application thereof. The structure of the compound is shown by formula (I). In-vitro competitive binding experiments indicate that the kind of molecules have medium affinity with the A(beta) 1-42 aggregate; in-vitro autoradiography experiments indicate that the molecules marked by Tc-99m can be combined with the A(beta) plaque in blood vessels of the brain with specificity and high affinity; in-vivo bio-distribution experiments on a normal mice indicate that a developer partially marked by Tc-99m has the advantages of low initial brain extraction, fast blood removal and the like, and is expected to become a new single-photon A(beta) plaque developer for early-stage clinical diagnosis of CAA (cerebral amyloid angiopathy) or AD (Alzheimer's disease).

99mTc-labeled benzothiazole and stilbene derivatives as imaging agents for Aβ plaques in cerebral amyloid angiopathy

β-Amyloid (Aβ) plaques in the blood vessels of the brain are associated with cerebral amyloid angiopathy (CAA), which is a common cause of stroke and vascular diseases. Imaging agents that can differentiate between Aβ plaques in the brain and those on the walls of cerebrovascular vessels will provide non-invasive biomarkers to interrogate the pathogenesis of CAA and give insights into the mechanisms, significance and impact of Aβ-CAA for developing effective therapies for CAA and stroke. A new series of 99mTc-labeled benzothiazole and stilbene derivatives with positive charge were developed and evaluated for selectively targeting Aβ plaques in the blood vessels of the brain. The rhenium complexes 6, 7, 13 and 14 displayed medium binding affinity to Aβ1-42 aggregates with Ki values of 162, 37, 366 and 78 nM, respectively. In vitro fluorescence staining of 7 and 14 demonstrated an intense labeling of Aβ plaques associated with blood vessel walls on brain sections of a patient with Alzheimer's diseases. A relatively low initial brain uptake for [99mTc]7 and [ 99mTc]14, 0.18 and 0.24 ID% per gram, respectively, suggests that they may be useful SPECT imaging agents for selectively detecting Aβ plaques associated with cerebral vessels in the living human brain.