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Cyclopentadienyl technetium ( 99m Tc) tricarbonyl piperidine conjugates: biodistribution and imaging studies
Author(s) -
Saidi Mouldi,
Kothari K.,
Pillai M. R. A.,
Hassan Amri,
Sarma H. D.,
Chaudhari P. R.,
Unnikrishnan T. P.,
Korde A.,
Azzouz Zohra
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.491
Subject(s) - chemistry , biodistribution , radiosynthesis , amine gas treating , piperidine , carboxylate , solvent , acetonitrile , technetium , radiochemistry , isopropyl , technetium 99m , nuclear chemistry , medicinal chemistry , stereochemistry , chromatography , organic chemistry , nuclear medicine , scintigraphy , positron emission tomography , medicine , biochemistry , in vitro
Synthesis of organometallic complexes of 99m Tc using the precursor ligands N ‐methylpiperidino‐4[(bispentahaptocyclopentadienyl)iron] carboxylate and N ‐(isopropyl)‐piperidino‐4[(bispentahaptocyclopentadienyl)iron]carboxylate is described. The labelling method involved reaction of the ligands with 99m TcO − 4in the presence of Mn(CO) 5 Br in dimethyl formamide at 150°C for 1 h in an oil bath. The purification of the complexes was carried out by preparative TLC using ethery/ n ‐butyl methyl amine (95:5) solvent system. The purified complexes were characterized by HPLC using acetonitrile:water (80:20) solvent system in a PRP‐1 column in which both the complexes were eluted as single peaks. Biodistribution studies carried out in rats showed 2.4±0.14 and 1.1±0.42% of the injected activity in the brain tissue 5 min p.i. for cytectrene I and II, respectively. The brain to blood activity ratio was >15:1 for both the complexes at 5 min p.i. Scintigraphic studies in rabbits showed significant uptake of the activity in the brain with fast clearance from blood. The complexes warrant further investigation as agents for brain imaging. Copyright © 2001 John Wiley & Sons, Ltd.