A fluorescent molecular imaging probe with selectivity for soluble tau aggregated protein.

Soluble forms of aggregated tau misfolded protein, generally termed oligomers, are considered to be the most toxic species of the different assembly states that are the pathological components of neurodegenerative disorders. Therefore, a critical biomedical need exists for imaging probes that can identify and quantify them. We have designed and synthesized a novel fluorescent probe, for which binding and selectivity profiles towards aggregated tau and Aβ proteins were assessed.

Direct Incorporation of [C]CO into Asymmetric [C]Carbonates.

A novel carbon-11 radiolabelling methodology for the synthesis of the dialkylcarbonate functional group has been developed. The method uses cyclotron-produced short-lived [C]CO (half-life 20.4 min) directly from the cyclotron target in a one-pot synthesis.

[(11)C]CO2 to [(11)C]CO conversion mediated by [(11)C]silanes: a novel route for [(11)C]carbonylation reactions.

A novel chemical methodology is described for the conversion of [(11)C]CO2 to [(11)C]CO. Diphenylmethyl silanes trap [(11)C]CO2 and release [(11)C]CO rapidly when triggered by TBAF. Released [(11)C]CO was used to produce [(11)C]N-benzylbenzamide and AMPA receptor ligand, [(11)C], in radiochemical yields >90% within 6 min from [(11)C]CO2 production.

Rapid and efficient synthesis of [11C]ureas via the incorporation of [11C]CO2 into aliphatic and aromatic amines.

A rapid urea radiolabelling methodology has been developed. [(11)C]CO2 was activated by 1,8-diazabicycloundec-7-ene (DBU) in the presence of aliphatic and aromatic amines and reacted with Mitsunobu reagents to produce asymmetric (11)C radiolabelled ureas in high radiochemical yields.