Chemical and radiopharmaceutical studies of technetium containing complexes
thesisposted on 2013-12-06, 09:38 authored by G.F.E. Morgan
The work described within this thesis takes the form of several different but related projects. The radionuclide, 99mTc, is widely used in nuclear medicine departments and researched in many laboratories throughout the world today and it is the intention of this thesis to contribute to the growing library of knowledge in this field. In chapter three, the technetium complex of tiron, a disulphonato derivative of catechol, is assessed for its radiopharmaceutical efficacy using both animal and human models. The no carrier added [ 99mTc] Tctiron preparation appears to form a single radiochemical species under the reaction conditions described, thought to be [99mTc] [TcO (tiron) 2,] s·-, based on the known reaction of technetium with catechol. A small highly charged ion could be expected to clear efficiently through the renal system, an expectation upheld by the animal studies and not observed in the human studies, where it is heavily protein bound. Chapters four and five are both concerned with thioether complexes of technetium, a donor group little studied with this particular metal. Firstly, a series of dithiadicarboxylic acids were synthesised or purchased and their subsequent reactions at both no carrier added [99mTc] and carrier added [99Tec] levels are discussed. Secondly, a macrocycle, potentially hexadentate through a S4 N2, donor set, was synthesised and derivatised and the reactions of these ligands with 99mTc and 99Tc are examined. In both cases, comprehensive animal studies are performed using two types of rodent, which show mixed hepatobiliary and renal clearance. [Continues...].