Synthesis and evaluation of ether containing 99mTc-nitrido dithiocarbamate complexes as brain perfusion imaging agent.
In the present study, a series of (99m)Tc-nitrido dithiocarbamate complexes containing ether linkages have been prepared and their brain perfusion characteristics studied. Two primary dithiocarbamates and two secondary dithiocarbamates were synthesized in >80% yield and were characterized by elemental analyses. The ligands were then labeled using a (99m)Tc-nitrido intermediate, prepared from sodium pertechnetate using commercially available nitrido kit-vials, at a low ligand concentration of 0.1 mg. The prepared complexes were obtained in more than 95% yield and were characterized by paper electrophoresis and HPLC. All the complexes were found to be neutral and eluted out as a single species in HPLC. Biodistribution studies were carried out in normal Swiss mice. All the complexes showed uptake in the brain. (99m)TcN complexes of secondary dithiocarbamates showed higher initial brain uptake (5 min p.i.) than their primary amine counterparts. However, all the complexes exhibited rapid washout from the brain.
Mallia
Madhava B
MB
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai 400085, India.
Mathur
Anupam
A
Subramanian
Suresh
S
Banerjee
Sharmila
S
Kothari
Kanchan
K
Koiry
S P
SP
Sarma
H D
HD
Venkatesh
Meera
M
D000818:Animals; D001783:Blood Flow Velocity; D001921:Brain / Q000098:blood supply* / Q000000981:diagnostic imaging*; D004353:Drug Evaluation, Preclinical; D004986:Ether / Q000737:chemistry / Q000493:pharmacokinetics*; D008657:Metabolic Clearance Rate; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D014018:Tissue Distribution
D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D004986:Ether