Rhenium and technetium complexes of thioamide derivatives of pyridylhydrazine that bind to amyloid- β plaques.

Rhenium and technetium complexes of thioamide derivatives of pyridylhydrazine that bind to amyloid-β plaques. J Biol Inorg Chem. 2018 Jul 07;: Authors: Fletcher SP, Noor A, Hickey JL, McLean CA, White JM, Donnelly PS Abstract Age-associated deposition of amyloid-β in cerebral blood vessels, a condition referred to as cerebral amyloid angiopathy, can contribute to stroke and dementia. This research aimed to design new radioactive technetium-99 m complexes that bind to amyloid-β plaques that have the potential to assist in diagnosis of cerebral amyloid angiopathy using single-photon-emitted computed tomography (SPECT) imaging. Six new pyridylthiosemicarbazide ligands containing either benzofuran or styrylpyridyl functional groups that are known to selectively bind to amyloid plaques were prepared. Non-radioactive isotopes of technetium are not available so rhenium was used as a surrogate for exploratory chemistry. The new ligands were used to prepare well-defined [Re-oxo]3+ complexes where two pyridylthiosemicarbazide ligands were coordinated to a single metal ion to give bivalent complexes with two amyloid-β targeting functional groups. The interaction of the [Re-oxo]3+ complexes with synthetic amyloid-β1-42 and with amyloid plaques in human brain tissue was investigated. Two ligands were selected to develop methods to prepare their [99mTc-oxo]3+ complexes at the tracer level. These technetium-99 m complexes are likely to be is...
Source: Journal of Biological Inorganic Chemistry : JBIC - Category: Chemistry Authors: Tags: J Biol Inorg Chem Source Type: research