Potential 67Ga radiopharmaceuticals for myocardial imaging: tris(1-aryl-3-hydroxy-2-methyl-4-pyridinonato)gallium(III) complexes.
A series of highly lipophilic complexes of 1-aryl-3-hydroxy-2-methyl-4-pyridinones with gallium(III)-67 has been evaluated in vitro and in vivo as potential radiopharmaceuticals. The pyridinones have different substituents at the para-position of the phenyl ring: R = H, CH3, OCH3 and NO2. Biodistribution studies of 67Ga complexes have been carried out in rabbits, mice, rats and a dog. High heart uptake of the radionuclide has been shown in rabbits and the dog. The different biodistribution patterns in mice and rats indicate that there is a species difference in the biodistribution of these complexes. Rabbits and the dog show rapid heart uptake and blood clearance. The speciation of the Ga3+ ion in vivo is simulated in vitro with a simple blood plasma model based on the available thermodynamic data.
Zhang
Z
Z
Department of Chemistry, University of British Columbia, Vancouver, Canada.
Lyster
D M
DM
Webb
G A
GA
Orvig
C
C
D000818:Animals; D002951:Citrates / Q000493:pharmacokinetics; D019343:Citric Acid; D003198:Computer Simulation; D004285:Dogs; D004355:Drug Stability; D005710:Gallium Radioisotopes; D006321:Heart / Q000000981:diagnostic imaging*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008954:Models, Biological; D009206:Myocardium / Q000378:metabolism; D009942:Organometallic Compounds / Q000493:pharmacokinetics; D011728:Pyridones / Q000493:pharmacokinetics; D011817:Rabbits; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D002951:Citrates; D005710:Gallium Radioisotopes; D009942:Organometallic Compounds; D011728:Pyridones; D019343:Citric Acid