Premium
Studies on 99m Tc complexes of functionalised propylene amine‐oxime (PnAO) ligands
Author(s) -
Pillai M. R. A.,
Kilcoin T.,
Kothari K.,
Ramamoorthy N.,
Lal Ramji,
Jurisson S. S.,
Schlemper E. O.
Publication year - 1999
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/(sici)1099-1344(199912)42:12<1161::aid-jlcr271>3.0.co;2-f
Subject(s) - chemistry , oxime , amine gas treating , bifunctional , biodistribution , ligand (biochemistry) , high performance liquid chromatography , elution , derivative (finance) , solvent , chromatography , solvent extraction , thin layer chromatography , stereochemistry , medicinal chemistry , extraction (chemistry) , organic chemistry , receptor , biochemistry , catalysis , economics , financial economics , in vitro
Three functionalised PnAO ligands, 3,3,9,9‐tetramethyl‐6‐R‐4, 8‐diazaundecane‐2,10‐dionedioxime (R=benzyl, p‐nitrobenzyl and p‐aminobenzyl) were synthesized. 99m Tc complexes of these ligands were prepared at both tracer levels and carrier added levels with 99m TcO − 4 and with 99 TcO − 4 . Complexation yields were estimated by thin layer chromatography, HPLC and solvent extraction studies. The complexes were formed in high yields; the resultant complexes were neutral, highly lipophilic (log P∽2.3–2.5) and elute as single peak on a reverse phase HPLC column. Complexes with all the three ligands showed excellent stability over 24 h period of storage at room temperature. Biodistribution studies of the 99m Tc complexes of the benzyl and nitrobenzyl ligands in Wistar rats showed brain uptake of 1.2±0.25% and 0.88±0.10% at 1 min post injection, respectively. The blood clearance was rapid in both the cases while the main excretory route was the hepatobiliary system. The aminobenzyl derivative is a bifunctional ligand which could be used for labeling antibodies and peptides with radiometals. Copyright © 1999 John Wiley & Sons, Ltd.