In the procurement of a neutral and compact monomeric complex of dithiosemicarbazone (DTS) derivative: 99mTc-KTS.
As a basic structure of a bifunctional radiopharmaceutical (BR), dithiosemicarbazone (DTS) enables the formation of a small conjugated chelating ring with divalent metals (Cu2+, Zn2+, Ni2+), yielding stable and compact complexes. In the development of a neutral and compact monomeric DTS complex of technetium (99mTc), a DTS containing ligand, kethoxal-bis(thiosemicarbazone) (KTS) was selected. A well known monomeric Cu-KTS complex (or 64Cu-KTS) is taken as a model compound, and in vitro (TLC, EP, HPLC) and in vivo (mice biodistribution) studies were compared. Using the stannous chloride method, under conditions to avoid the hydrolytic polynucleation of technetium, a good yield of 99mTc-KTS with characteristics resembling the non-charged, compact and stable Cu-KTS is obtained, in in vitro as well as in vivo studies. The importance of DTS as the constituent of a BR is discussed.
Hosotani
T
T
Yokoyama
A
A
Arano
Y
Y
Horiuchi
K
K
Wasaki
H
H
Saji
H
H
Torizuka
K
K
D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000378:metabolism; D003432:Cross-Linking Reagents / Q000138:chemical synthesis / Q000378:metabolism; D051379:Mice; D015609:Organotechnetium Compounds; D013667:Technetium / Q000138:chemical synthesis* / Q000378:metabolism; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000378:metabolism; D014018:Tissue Distribution
D002614:Chelating Agents; D003432:Cross-Linking Reagents; D015609:Organotechnetium Compounds; D013882:Thiosemicarbazones; C049201:kethoxal-bis(thiosemicarbazone)technetium complex; D013667:Technetium