Synthesis, characterization and biodistribution of new 99mTc oxo and nitrido complexes with bi- and tetradendate unsaturated NS and N2S2 Schiff bases derived from 2-aminocyclopentene-1-dithiocarboxylic acid as potential heart imaging agents.
The synthesis, characterization and 99mTc labelling of unsaturated diamino dithiol ligands with methyl dithiocarboxylate functions: 2-aminocyclopentene-1-dithiocarboxylic methyl ester (H2L1), N,N'-ethylene bis(methyl 2-aminocyclopentene-1-dithiocarboxylate) (H2L2) and N,N'-propylene bis (methyl 2-aminocyclopentene-1-dithiocarboxylate) (H2L3) are described. Cationic oxo (Tc = O) and neutral nitrido (Tc = N) complexes were obtained. Biodistribution studies in rat showed a good heart uptake of 99mTcN-L2 (2% ID at 5 min) with a high heart-to-blood ratio (5.8 at 5 min), but this complex also exhibited high lung and liver uptake.
Coulais
Y
Y
Laboratoire de Biophysique et de Médecine Nucléaire, Faculté de Médecine Toulouse-Purpan, France.
Cros
G
G
Darbieu
M H
MH
Tafani
J A
JA
Belhadj-Tahar
H
H
Bellande
E
E
Pasqualini
R
R
Guiraud
R
R
D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis*; D003517:Cyclopentanes / Q000138:chemical synthesis*; D006321:Heart / Q000000981:diagnostic imaging*; D007659:Ketones / Q000032:analysis / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D008024:Ligands; D008297:Male; D008970:Molecular Weight; D015609:Organotechnetium Compounds / Q000032:analysis / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000032:analysis / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D012545:Schiff Bases / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
C107952:2-aminocyclopentene-1-dithiocarboxylic acid; D002264:Carboxylic Acids; D003517:Cyclopentanes; D007659:Ketones; D008024:Ligands; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D012545:Schiff Bases