Novel Cyclopentadienyl Tricarbonyl Complexes of 99mTc Mimicking Chalcone as Potential Single-Photon Emission Computed Tomography Imaging Probes for β-Amyloid Plaques in Brain
摘要:
Rhenium and technetium-99m cyclopentadienyl tricarbonyl complexes mimicking the chalcone structure were prepared. These complexes were proved to have affinity to beta-amyloid (A beta) in fluorescent staining on brain sections of Alzheimer's Disease (AD) patient and binding assay using A beta(1-42) aggregates, with K-i values ranging from 899 to 108 nM as the extension of conjugated pi system. In vitro autoradiograpy on sections of transgenic mouse brain confirmed the affinity of [Tc-99m]5 (K-i = 108 nM). In biodistribution, all compounds showed good initial uptakes into the brain and fast blood clearance, while the decreasing of initial brain uptakes correspond to increasing of conjugation length, from 4.10 +/- 0.38% ID/g ([Tc-99m]3) to 1.11 +/- 0.34% ID/g ([Tc-99m]5). These small technetium-99m complexes (<500 Da) designed by an integrated approach provide encouraging evidence that development of a promising Tc-99m-labeled agent for imaging A beta plaques in the brain may be feasible.
Aqueous One-Pot Synthesis of Derivatized Cyclopentadienyl-Tricarbonyl Complexes of99mTc with an In Situ CO Source: Application to a Serotonergic Receptor Ligand
摘要:
Instant radiopharmaceuticals-just add [(99m) TcO4 ](-) in water! Half-sandwich complexes of the type [(RCOCp)(99m) Tc(CO)3 ] (e.g. 1) were synthesized in a single step in water from [(99m) TcO4 ](-) . The acidification of the Cp ring by a carbonyl substituent and the use of K2 [H3 BCO2 ] as a reducing agent and in situ source of CO are instrumental in the synthesis.