title: Synthesis and evaluation of technetium-99m monocationic mixed ligand complexes of phenyl substituted/condensed tetradentate Schiff's bases and trimethylphosphine.
abstract: Tc-99m monocationic mixed ligand complexes of phenyl substituted/condensed Schiff's bases, N,N'-ethylene-bis-(benzoylacetone imine) (Lb) or N,N'-ethylene-bis-(salicylaldehyde imine) (Lc) or N,N'-ethylene-bis-(2-hydroxyacetophenone imine) (Ld) and trimethylphosphine were synthesized to determine the influence of the presence of a phenyl group in these tracers on their heart uptake in rats. A new formulation procedure using aq. beta-hydroxypropylcyclodextrin (HPB) solution was developed for intravenous administration of nonpolar 99mTc complexes. Comparison of biodistribution data for the reference 99mTc complex from N,N'-ethylene-bis-(acetylacetone imine) and trimethylphosphine using HPB formulation and alternate formulation (0.9% saline) showed the same results. Biodistribution of the title 99mTc complexes, [99mTc Lb (PMe3)2]+, [99mTc Lc (PMe3)2]+ and [99mTc Ld (PMe3)2]+ showed heart-to-blood activity ratios of 1.7, 2.1 and 1.7, respectively, at 15 min post-injection in rats.
authors.affiliation: University of Texas Southwestern Medical Center, Dallas 75235-9058.
authors.forename: N C
authors.initials: NC
authors.lastname: Goomer
authors.forename: P V
authors.initials: PV
authors.lastname: Kulkarni
authors.forename: A
authors.initials: A
authors.lastname: Constantinescu
authors.forename: P
authors.initials: P
authors.lastname: Antich
authors.forename: R W
authors.initials: RW
authors.lastname: Parkey
authors.forename: J R
authors.initials: JR
authors.lastname: Corbett
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D003505:Cyclodextrins / Q000138:chemical synthesis; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D010720:Phosphines; D051381:Rats; D011919:Rats, Inbred Strains; D012545:Schiff Bases; D012996:Solutions; D014018:Tissue Distribution; D047392:beta-Cyclodextrins
chemical_list: D003505:Cyclodextrins; D015609:Organotechnetium Compounds; D010720:Phosphines; D012545:Schiff Bases; D012996:Solutions; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C049750:trimethyl phosphine