Technetium labeling of bi, tri and tetradentate ligands derived from 2-aminocyclopentene-1-dithiocarboxylic acid: characterization and biodistribution of their oxo and nitrido 99mtechnetium complexes.
We have synthesized and characterized seven ligands derived from 2-aminocyclopentene-1-dithiocarboxylic acid with different donor sets (SN2-, SNO2-, SNN2-, SNNO3- and SNNN3-) and different substituents on the sulfur moieties-SR (with R = H, CH3 or C2H5O(CH3)CH). With five of these ligands technetium nitrido complexes have been obtained with high yields (over 95%) using rather harsh conditions (pH = 1, temperature > or = 80 degrees C), whereas for technetium oxo complexes similar high yields were only obtained with two ligands but with mild conditions (pH = 7-8, temperature approximately equal to 50 degrees C). Changing an OH group for an NH2 has a drastic effect upon labeling yields. The possibility of complexing ligands as either oxo (TcO)3+ or nitrido (TcN)2+ derivatives increases the number of available labeled agents with different overall change and consequently with different biological behavior.
Belhadj-Tahar
H
H
Laboratoire D'imagerie Morphologique et Fonctionnelle, Faculté de Medecine Toulouse-Purpan, France.
Coulais
Y
Y
Cros
G
G
Darbieu
M H
MH
Tafani
J A
JA
Fabre
J
J
Esquerré
J P
JP
Guiraud
R
R
D000818:Animals; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013667:Technetium / Q000493:pharmacokinetics; D013871:Thiones / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014961:X-Ray Diffraction
D008024:Ligands; D013871:Thiones; D013667:Technetium