Synthesis and bio-evaluation of a new fatty acid derivative for myocardial imaging.
Development of a (99m)Tc-fatty acid analogue is of interest, as (99m)Tc is logistically advantageous over the cyclotron-produced (11)C and (123)I. Synthesis of a 16 carbon fatty acid derivative and its radiolabeling with the novel [(99m)TcN(PNP)](2+) core is described here. Hexadecanedioic acid was conjugated to cysteine in an overall yield of 55%. This ligand could be labeled with (99m)Tc via the [(99m)TcN(PNP)](2+) core, in 80% yield, as a mixture of two isomers (syn and anti). The major isomer isolated by HPLC was used for bioevaluation studies in swiss mice and compared with radioiodinated iodophenyl pentadecanoic acid (IPPA), an established agent for myocardial metabolic imaging. (99m)Tc-labeled complex cleared faster from the non-target organs, namely, liver, lungs, and blood compared to that of [(125)I]-IPPA. However, the complex exhibited lower uptake and faster washout from the myocardium as compared to [(125)I]-IPPA.
Mathur
Anupam
A
Radiopharmaceuticals Program, Board of Radiation and Isotope Technology, Mumbai 400705, India.
Subramanian
Suresh
S
Mallia
Madhava B
MB
Banerjee
Sharmila
S
Samuel
Grace
G
Sarma
Haladhar D
HD
Venkatesh
Meera
M
D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D003545:Cysteine / Q000737:chemistry; D005227:Fatty Acids / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D006321:Heart / Q000000981:diagnostic imaging*; D007457:Iodine Radioisotopes; D007462:Iodobenzenes / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics; D007553:Isotope Labeling; D008024:Ligands; D008657:Metabolic Clearance Rate; D051379:Mice; D015394:Molecular Structure; D009206:Myocardium / Q000378:metabolism*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D010169:Palmitic Acids / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D012680:Sensitivity and Specificity; D013237:Stereoisomerism; D013997:Time Factors; D014018:Tissue Distribution
D005227:Fatty Acids; D007457:Iodine Radioisotopes; D007462:Iodobenzenes; D008024:Ligands; D015609:Organotechnetium Compounds; D010169:Palmitic Acids; C012346:hexadecanedioic acid; C025391:omega-(4-iodophenyl)pentadecanoic acid; D003545:Cysteine